Items where Author is "Wittlin, S."

2023

Nguyen, W. and Dans, M. G. and Currie, I. and Awalt, J. K. and Bailey, B. L. and Lumb, C. and Ngo, A. and Favuzza, P. and Palandri, J. and Ramesh, S. and Penington, J. and Jarman, K. E. and Mukherjee, P. and Chakraborty, A. and Maier, A. G. and van Dooren, G. G. and Papenfuss, T. and Wittlin, S. and Churchyard, A. and Baum, J. and Winzeler, E. A. and Baud, D. and Brand, S. and Jackson, P. F. and Cowman, A. F. and Sleebs, B. E.. (2023) 7-N-substituted-3-oxadiazole quinolones with potent antimalarial activity target the cytochrome bc1 complex. ACS Infect Dis, 9 (3). pp. 668-691.

Imlay, L. S. and Lawong, A. K. and Gahalawat, S. and Kumar, A. and Xing, C. and Mittal, N. and Wittlin, S. and Churchyard, A. and Niederstrasser, H. and Crespo-Fernandez, B. and Posner, B. A. and Gamo, F. J. and Baum, J. and Winzeler, E. A. and Laleu, B. and Ready, J. M. and Phillips, M. A.. (2023) Fast-killing tyrosine amide ((S)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance locus (PfCARL). ACS Infect Dis, 9 (3). pp. 527-539.

Walz, A. and Duffey, M. and Aljayyoussi, G. and Sax, S. and Leroy, D. and Besson, A. and Burrows, J. N. and Cherkaoui-Rbati, M. H. and Gobeau, N. and Westwood, M.-A. and Siethoff, C. and Gamo, S. and Mäser, P. and Wittlin, S.. (2023) The Parasite Reduction Ratio (PRR) assay version 2: standardized assessment of Plasmodium falciparum viability after antimalarial treatment in vitro. Pharmaceuticals (Basel), 16 (2). p. 163.

Davies, H. and Bergmann, B. and Walloch, P. and Nerlich, C. and Hansen, C. and Wittlin, S. and Spielmann, T. and Treeck, M. and Beitz, E.. (2023) The plasmodium lactate/H+ transporter PfFNT is essential and druggable in vivo. Antimicrob Agents Chemother, 67 (8). e0035623.

2022

Lowe, M. A. and Cardenas, A. and Valentin, J. P. and Zhu, Z. and Abendroth, J. and Castro, J. L. and Class, R. and Delaunois, A. and Fleurance, R. and Gerets, H. and Gryshkova, V. and King, L. and Lorimer, D. D. and MacCoss, M. and Rowley, J. H. and Rosseels, M. L. and Royer, L. and Taylor, R. D. and Wong, M. and Zaccheo, O. and Chavan, V. P. and Ghule, G. A. and Tapkir, B. K. and Burrows, J. N. and Duffey, M. and Rottmann, M. and Wittlin, S. and Angulo-Barturen, I. and Jiménez-Díaz, M. B. and Striepen, J. and Fairhurst, K. J. and Yeo, T. and Fidock, D. A. and Cowman, A. F. and Favuzza, P. and Crespo-Fernandez, B. and Gamo, F. J. and Goldberg, D. E. and Soldati-Favre, D. and Laleu, B. and de Haro, T.. (2022) Discovery and characterization of potent, efficacious, orally available antimalarial plasmepsin X inhibitors and preclinical safety assessment of UCB7362. Journal of medicinal chemistry, 65 (20). pp. 14121-14143.

Laleu, B. and Rubiano, K. and Yeo, T. and Hallyburton, I. and Anderson, M. and Crespo-Fernandez, B. and Gamo, F. J. and Antonova-Koch, Y. and Orjuela-Sanchez, P. and Wittlin, S. and Jana, G. P. and Maity, B. C. and Chenu, E. and Duffy, J. and Sjo, P. and Waterson, D. and Winzeler, E. and Guantai, E. and Fidock, D. A. and Hansson, T.. (2022) Exploring a tetrahydroquinoline antimalarial hit from the medicines for malaria pathogen box and the identification of its mode of resistance as PfeEF2. ChemMedChem, 17 (22). e202200393.

Dong, Y. and Sonawane, Y. and Maher, S. P. and Zeeman, A. M. and Chaumeau, V. and Vantaux, A. and Cooper, C. A. and Chiu, F. C. K. and Ryan, E. and McLaren, J. and Chen, G. and Wittlin, S. and Witkowski, B. and Nosten, F. and Sriraghavan, K. and Kyle, D. E. and Kocken, C. H. M. and Charman, S. A. and Vennerstrom, J. L.. (2022) Metabolic, pharmacokinetic, and activity profile of the liver stage antimalarial (RC-12). ACS Omega, 7 (14). pp. 12401-12411.

Mambwe, D. and Korkor, CM. and Mabhula, A. and Ngqumba, Z. and Cloete, C. and Kumar, M. and Barros, PL. and Leshabane, M. and Coertzen, D. and Taylor, D. and Gibhard, L. and Njoroge, M. and Lawrence, N. and Reader, J. and Moreira, DR. and Birkholtz, LM. and Wittlin, S. and Egan, TJ. and Chibale, K.. (2022) Novel 3-trifluoromethyl-1,2,4-oxadiazole analogues of astemizole with multi-stage antiplasmodium activity and; in vivo; efficacy in a; Plasmodium berghei; mouse malaria infection model. Journal of medicinal chemistry, 65 (24). pp. 16695-16715.

de Vries, L. E. and Jansen, P. A. M. and Barcelo, C. and Munro, J. and Verhoef, J. M. J. and Pasaje, C. F. A. and Rubiano, K. and Striepen, J. and Abla, N. and Berning, L. and Bolscher, J. M. and Demarta-Gatsi, C. and Henderson, R. W. M. and Huijs, T. and Koolen, K. M. J. and Tumwebaze, P. K. and Yeo, T. and Aguiar, A. C. C. and Angulo-Barturen, I. and Churchyard, A. and Baum, J. and Fernandez, B. C. and Fuchs, A. and Gamo, F. J. and Guido, R. V. C. and Jimenez-Diaz, M. B. and Pereira, D. B. and Rochford, R. and Roesch, C. and Sanz, L. M. and Trevitt, G. and Witkowski, B. and Wittlin, S. and Cooper, R. A. and Rosenthal, P. J. and Sauerwein, R. W. and Schalkwijk, J. and Hermkens, P. H. H. and Bonnert, R. V. and Campo, B. and Fidock, D. A. and Llinas, M. and Niles, J. C. and Kooij, T. W. A. and Dechering, K. J.. (2022) Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183. Nat Commun, 13. p. 2158.

Xie, S. C. and Metcalfe, R. D. and Dunn, E. and Morton, C. J. and Huang, S. C. and Puhalovich, T. and Du, Y. and Wittlin, S. and Nie, S. and Luth, M. R. and Ma, L. and Kim, M. S. and Pasaje, C. F. A. and Kumpornsin, K. and Giannangelo, C. and Houghton, F. J. and Churchyard, A. and Famodimu, M. T. and Barry, D. C. and Gillett, D. L. and Dey, S. and Kosasih, C. C. and Newman, W. and Niles, J. C. and Lee, M. C. S. and Baum, J. and Ottilie, S. and Winzeler, E. A. and Creek, D. J. and Williamson, N. and Parker, M. W. and Brand, S. and Langston, S. P. and Dick, L. R. and Griffin, M. D. W. and Gould, A. E. and Tilley, L.. (2022) Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy. Science, 376 (6597). pp. 1074-1079.

2021

Knaab, T. C. and Held, J. and Burckhardt, B. B. and Rubiano, K. and Okombo, J. and Yeo, T. and Mok, S. and Uhlemann, A. C. and Lungerich, B. and Fischli, C. and Pessanha de Carvalho, L. and Mordmüller, B. and Wittlin, S. and Fidock, D. A. and Kurz, T.. (2021) 3-Hydroxy-propanamidines, a new class of orally active antimalarials targeting Plasmodium falciparum. Journal of medicinal chemistry, 64 (6). pp. 3035-3047.

Dziwornu, G. A. and Coertzen, D. and Leshabane, M. and Korkor, C. M. and Cloete, C. K. and Njoroge, M. and Gibhard, L. and Lawrence, N. and Reader, J. and van der Watt, M. and Wittlin, S. and Birkholtz, L. M. and Chibale, K.. (2021) Antimalarial benzimidazole derivatives incorporating phenolic mannich base side chains inhibit microtubule and hemozoin formation: structure-activity relationship and in vivo oral efficacy studies. Journal of medicinal chemistry, 64 (8). pp. 5198-5215.

Shackleford, D. M. and Chiu, F. C. K. and Katneni, K. and Blundell, S. and McLaren, J. and Wang, X. and Zhou, L. and Sriraghavan, K. and Alker, A. M. and Hunziker, D. and Scheurer, C. and Zhao, Q. and Dong, Y. and Mohrle, J. J. and Abla, N. and Matile, H. and Wittlin, S. and Vennerstrom, J. L. and Charman, S. A.. (2021) Cytochrome P450-mediated metabolism and CYP Inhibition for the synthetic peroxide antimalarial OZ439. ACS Infect Dis, 7 (7). pp. 1885-1893.

Xie, S. C. and Metcalfe, R. D. and Mizutani, H. and Puhalovich, T. and Hanssen, E. and Morton, C. J. and Du, Y. and Dogovski, C. and Huang, S. C. and Ciavarri, J. and Hales, P. and Griffin, R. J. and Cohen, L. H. and Chuang, B. C. and Wittlin, S. and Deni, I. and Yeo, T. and Ward, K. E. and Barry, D. C. and Liu, B. and Gillett, D. L. and Crespo-Fernandez, B. F. and Ottilie, S. and Mittal, N. and Churchyard, A. and Ferguson, D. and Aguiar, A. C. C. and Guido, R. V. C. and Baum, J. and Hanson, K. K. and Winzeler, E. A. and Gamo, F. J. and Fidock, D. A. and Baud, D. and Parker, M. W. and Brand, S. and Dick, L. R. and Griffin, M. D. W. and Gould, A. E. and Tilley, L.. (2021) Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome. Proc Natl Acad Sci U S A, 118 (39). e2107213118.

Leas, D. A. and Sanford, A. G. and Wu, J. and Cal, M. and Kaiser, M. and Wittlin, S. and Hemsley, R. M. and Darner, E. B. and Lui, L. M. and Davis, P. H. and Vennerstrom, J. L.. (2021) Diaryl ureas as an antiprotozoal chemotype. ACS Infect Dis, 7 (6). pp. 1578-1583.

Laleu, B. and Akao, Y. and Ochida, A. and Duffy, S. and Lucantoni, L. and Shackleford, D. M. and Chen, G. and Katneni, K. and Chiu, F. C. K. and White, K. L. and Chen, X. and Sturm, A. and Dechering, K. J. and Crespo, B. and Sanz, L. M. and Wang, B. and Wittlin, S. and Charman, S. A. and Avery, V. M. and Cho, N. and Kamaura, M.. (2021) Discovery and structure-activity relationships of quinazolinone-2-carboxamide derivatives as novel orally efficacious antimalarials. Journal of medicinal chemistry, 64 (17). pp. 12582-12602.

Wittlin, S. and Mäser, P.. (2021) From magic bullet to magic bomb: reductive bioactivation of antiparasitic agents. ACS Infect Dis, 7 (10). pp. 2777-2786.

Le Manach, C. and Dam, J. and Woodland, J. G. and Kaur, G. and Khonde, L. P. and Brunschwig, C. and Njoroge, M. and Wicht, K. J. and Horatscheck, A. and Paquet, T. and Boyle, G. A. and Gibhard, L. and Taylor, D. and Lawrence, N. and Yeo, T. and Mok, S. and Eastman, R. T. and Dorjsuren, D. and Talley, D. C. and Guo, H. and Simeonov, A. and Reader, J. and van der Watt, M. and Erlank, E. and Venter, N. and Zawada, J. W. and Aswat, A. and Nardini, L. and Coetzer, T. L. and Lauterbach, S. B. and Bezuidenhout, B. C. and Theron, A. and Mancama, D. and Koekemoer, L. L. and Birkholtz, L. M. and Wittlin, S. and Delves, M. and Ottilie, S. and Winzeler, E. A. and von Geldern, T. W. and Smith, D. and Fidock, D. A. and Street, L. J. and Basarab, G. S. and Duffy, J. and Chibale, K.. (2021) Identification and profiling of a novel diazaspiro[3.4]octane chemical series active against multiple stages of the human malaria parasite Plasmodium falciparum and optimization efforts. Journal of medicinal chemistry, 64 (4). pp. 2291-2309.

Cheuka, P. M. and Centani, L. and Arendse, L. B. and Fienberg, S. and Wambua, L. and Renga, S. S. and Dziwornu, G. A. and Kumar, M. and Lawrence, N. and Taylor, D. and Wittlin, S. and Coertzen, D. and Reader, J. and van der Watt, M. and Birkholtz, L. M. and Chibale, K.. (2021) New amidated 3,6-diphenylated imidazopyridazines with potent antiplasmodium activity are dual inhibitors of; Plasmodium; phosphatidylinositol-4-kinase and cGMP-dependent protein kinase. ACS Infect Dis, 7 (1). pp. 34-46.

Lawong, A. and Gahalawat, S. and Okombo, J. and Striepen, J. and Yeo, T. and Mok, S. and Deni, I. and Bridgford, J. L. and Niederstrasser, H. and Zhou, A. and Posner, B. and Wittlin, S. and Gamo, F. J. and Crespo, B. and Churchyard, A. and Baum, J. and Mittal, N. and Winzeler, E. and Laleu, B. and Palmer, M. J. and Charman, S. A. and Fidock, D. A. and Ready, J. M. and Phillips, M. A.. (2021) Novel antimalarial tetrazoles and amides active against the hemoglobin degradation pathway in Plasmodium falciparum. Journal of medicinal chemistry, 64 (5). pp. 2739-2761.

Boss, C. and Wittlin, S.. (2021) Our exciting journey to ACT-451840. Chimia, 75 (11). pp. 916-922.

Palmer, M. J. and Deng, X. and Watts, S. and Krilov, G. and Gerasyuto, A. and Kokkonda, S. and El Mazouni, F. and White, J. and White, K. L. and Striepen, J. and Bath, J. and Schindler, K. A. and Yeo, T. and Shackleford, D. M. and Mok, S. and Deni, I. and Lawong, A. and Huang, A. and Chen, G. and Wang, W. and Jayaseelan, J. and Katneni, K. and Patil, R. and Saunders, J. and Shahi, S. P. and Chittimalla, R. and Angulo-Barturen, I. and Jimenez-Diaz, M. B. and Wittlin, S. and Tumwebaze, P. K. and Rosenthal, P. J. and Cooper, R. A. and Aguiar, A. C. C. and Guido, R. V. C. and Pereira, D. B. and Mittal, N. and Winzeler, E. A. and Tomchick, D. R. and Laleu, B. and Burrows, J. N. and Rathod, P. K. and Fidock, D. A. and Charman, S. A. and Phillips, M. A.. (2021) Potent antimalarials with development potential identified by structure-guided computational optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series. Journal of medicinal chemistry, 64 (9). pp. 6085-6136.

Okaniwa, M. and Shibata, A. and Ochida, A. and Akao, Y. and White, K. L. and Shackleford, D. M. and Duffy, S. and Lucantoni, L. and Dey, S. and Striepen, J. and Yeo, T. and Mok, S. and Aguiar, A. C. C. and Sturm, A. and Crespo, B. and Sanz, L. M. and Churchyard, A. and Baum, J. and Pereira, D. B. and Guido, R. V. C. and Dechering, K. J. and Wittlin, S. and Uhlemann, A. C. and Fidock, D. A. and Niles, J. C. and Avery, V. M. and Charman, S. A. and Laleu, B.. (2021) Repositioning and characterization of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives as Plasmodium cytoplasmic prolyl-trna synthetase inhibitors. ACS Infect Dis, 7 (6). pp. 1680-1689.

Hitz, E. and Wiedemar, N. and Passecker, A. and Graça, B. A. S. and Scheurer, C. and Wittlin, S. and Brancucci, N. M. B. and Vakonakis, I. and Mäser, P. and Voss, T. S.. (2021) The 3-phosphoinositide-dependent protein kinase 1 is an essential upstream activator of protein kinase A in malaria parasites. PLoS Biol, 19 (12). e3001483.

Murithi, J. M. and Pascal, C. and Bath, J. and Boulenc, X. and Gnadig, N. F. and Pasaje, C. F. A. and Rubiano, K. and Yeo, T. and Mok, S. and Klieber, S. and Desert, P. and Jimenez-Diaz, M. B. and Marfurt, J. and Rouillier, M. and Cherkaoui-Rbati, M. H. and Gobeau, N. and Wittlin, S. and Uhlemann, A. C. and Price, R. N. and Wirjanata, G. and Noviyanti, R. and Tumwebaze, P. and Cooper, R. A. and Rosenthal, P. J. and Sanz, L. M. and Gamo, F. J. and Joseph, J. and Singh, S. and Bashyam, S. and Augereau, J. M. and Giraud, E. and Bozec, T. and Vermat, T. and Tuffal, G. and Guillon, J. M. and Menegotto, J. and Salle, L. and Louit, G. and Cabanis, M. J. and Nicolas, M. F. and Doubovetzky, M. and Merino, R. and Bessila, N. and Angulo-Barturen, I. and Baud, D. and Bebrevska, L. and Escudie, F. and Niles, J. C. and Blasco, B. and Campbell, S. and Courtemanche, G. and Fraisse, L. and Pellet, A. and Fidock, D. A. and Leroy, D.. (2021) The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance. Sci Transl Med, 13 (603). eabg6013.

Hitz, E. and Grüninger, O. and Passecker, A. and Wyss, M. and Scheurer, C. and Wittlin, S. and Beck, H. P. and Brancucci, N. M. B. and Voss, T. S.. (2021) The catalytic subunit of Plasmodium falciparum casein kinase 2 is essential for gametocytogenesis. Commun Biol, 4 (1). p. 336.

2020

Ahenkorah, S. and Coertzen, D. and Tong, J. X. and Fridianto, K. and Wittlin, S. and Birkholtz, L. M. and Tan, K. S. W. and Lam, Y. and Go, M. L. and Haynes, R. K.. (2020) Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships. ACS medicinal chemistry letters, 11. pp. 49-55.

Potluri, V. and Shandil, R. K. and Gavara, R. and Sambasivam, G. and Campo, B. and Wittlin, S. and Narayanan, S.. (2020) Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J, 19. p. 365.

Horatscheck, A. and Andrijevic, A. and Nchinda, A. T. and Le Manach, C. and Paquet, T. and Khonde, L. P. and Dam, J. and Pawar, K. and Taylor, D. and Lawrence, N. and Brunschwig, C. and Gibhard, L. and Njoroge, M. and Reader, J. and van der Watt, M. and Wicht, K. and de Sousa, A. C. C. and Okombo, J. and Maepa, K. and Egan, T. J. and Birkholtz, L. M. and Basarab, G. S. and Wittlin, S. and Fish, P. V. and Street, L. J. and Duffy, J. and Chibale, K.. (2020) Identification of 2,4-disubstituted imidazopyridines as hemozoin formation inhibitors with fast-killing kinetics and in vivo efficacy in the Plasmodium falciparum NSG mouse model. Journal of medicinal chemistry, 63 (21). pp. 13013-13030.

2019

Walz, A. and Leroy, D. and Andenmatten, N. and Mäser, P. and Wittlin, S.. (2019) Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay. Malaria journal, 18. p. 427.

Krieg, R. and Jortzik, E. and Goetz, A. A. and Blandin, S. and Wittlin, S. and Elhabiri, M. and Rahbari, M. and Nuryyeva, S. and Voigt, K. and Dahse, H. M. and Brakhage, A. and Beckmann, S. and Quack, T. and Grevelding, C. G. and Pinkerton, A. B. and Schonecker, B. and Burrows, J. and Davioud-Charvet , E. and Rahlfs, S. and Becker, K.. (2019) Author correction: Arylmethylamino steroids as antiparasitic agents. Nature Communications, 10. p. 2997.

Baartzes, N. and Stringer, T. and Seldon, R. and Warner, D. F. and Taylor, D. and Wittlin, S. and Chibale, K. and Smith, G. S.. (2019) Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids : antimicrobial evaluation and mechanistic insights. European journal of medicinal chemistry, 180. pp. 121-133.

Attram, H. D. and Wittlin, S. and Chibale, K.. (2019) Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles. MedChemComm , 10 (3). pp. 450-455.

Hooft van Huijsduijnen, R. and Wells, T. and Tanner, M. and Wittlin, S.. (2019) Two successful decades of Swiss collaborations to develop new anti-malarials. Malaria journal, 18. p. 94.

2018

Cheuka, P. M. and Larence, N. and Taylor, D. and Wittlin, S. and Chibale, K.. (2018) Antiplasmodial imidazopyridazines : structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles. MedChemComm , 9 (10). pp. 1733-1745.

Boss, C. and Wittlin, S.. (2018) Recent trends in malaria research. In: 2018 Medicinal chemistry reviews: from the medicinal chemistry division of the ACS, 53. Minneapolis, pp. 293-311.

2017

Pavadai, E. and Kaur, G. and Wittlin, S. and Chibale, K.. (2017) Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening. MedChemComm , 8 (6). pp. 1152-1157.

2015

Kaur, G. and Singh, K. and Pavadai, E. and Njoroge, M. and Espinoza-Moraga, M. and de Kock, C. and Smith, P. J. and Wittlin, S. and Chibale, K.. (2015) Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G. MedChemComm, 6 (11). pp. 2023-2028.

2013

Wang, X. and Dong, Y. and Wittlin, S. and Charman, S. A. and Chiu, F. C. and Chollet, J. and Katneni, K. and Mannila, J. and Morizzi, J. and Ryan, E. and Scheurer, C. and Steuten, J. and Santo, Tomas J. and Snyder, C. and Vennerstrom, J. L.. (2013) Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. Journal of medicinal chemistry, 56 (6). pp. 2547-2555.

Moehrle, J. J. and Duparc, S. and Siethoff, C. and van Giersbergen, P. L. and Craft, J. C. and Arbe-Barnes, S. and Charman, S. A. and Gutierrez, M. and Wittlin, S. and Vennerstrom, J. L.. (2013) First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials. British journal of clinical pharmacology, Vol. 75, H. 2. pp. 535-548.

Ciana, C. L. and Siegrist, R. and Aissaoui, H. and Marx, L. and Racine, S. and Meyer, S. and Binkert, C. and de Kanter, R. and Fischli, C. and Wittlin, S. and Boss, C.. (2013) Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold. Bioorganic & medicinal chemistry letters : a Tetrahedron publication for the rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Vol. 23, H. 3. pp. 658-662.

Brunner, R. and Ng, C. L. and Aissaoui, H. and Akabas, M. H. and Boss, C. and Brun, R. and Callaghan, P. S. and Corminboeuf, O. and Fidock, D. A. and Frame, I. J. and Heidmann, B. and Le Bihan, A. and Jeno, P. and Mattheis, C. and Moes, S. and Muller, I. B. and Paguio, M. and Roepe, P. D. and Siegrist, R. and Voss, Till S. and Welford, R. W. and Wittlin, S. and Binkert, C.. (2013) UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells. Journal of biological chemistry, Vol. 288, H. 31. pp. 22576-22583.

2012

Younis, Y. and Douelle, F. and Feng, T. S. and Cabrera, D. G. and Manach, C. L. and Nchinda, A. T. and Duffy, S. and White, K. L. and Shackleford, D. M. and Morizzi, J. and Mannila, J. and Katneni, K. and Bhamidipati, R. and Zabiulla, K. M. and Joseph, J. T. and Bashyam, S. and Waterson, D. and Witty, M. J. and Hardick, D. and Wittlin, S. and Avery, V. and Charman, S. A. and Chibale, K.. (2012) 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. Journal of medicinal chemistry, 55 (7). pp. 3479-3487.

Li, Y. and Wittlin, S. and Wu, Y.. (2012) Access to some UV chromophore-containing antimalarial trioxanes using hydrogen peroxide as source of the peroxy bonds. Heterocycles : an international journal for reviews and communications in heterocyclic chemistry, Vol. 84, H. 2. pp. 1217-1226.

Mäser, P. and Wittlin, S. and Rottmann, M. and Wenzler, T. and Kaiser, M. and Brun, R.. (2012) Antiparasitic agents : new drugs on the horizon. Current opinion in pharmacology, Vol. 12, H. 5. pp. 562-566.

Marfurt, J. and Chalfein, F. and Prayoga, P. and Wabiser, F. and Wirjanata, G. and Sebayang, B. and Piera, K. A. and Wittlin, S. and Haynes, R. K. and Mohrle, J. J. and Anstey, N. M. and Kenangalem, E. and Price, R. N.. (2012) Comparative ex vivo activity of novel endoperoxides in multidrug-resistant Plasmodium falciparum and P. vivax. Antimicrobial agents and chemotherapy : AAC, Vol. 56, H. 10. pp. 5258-5263.

Edlin, C. D. and Morgans, G. and Winks, S. and Duffy, S. and Avery, V. M. and Wittlin, S. and Waterson, D. and Burrows, J. and Bryans, J.. (2012) Identification and in-vitro ADME assessment of a series of novel anti-malarial agents suitable for hit-to-lead chemistry. ACS medicinal chemistry letters, Vol. 3, H. 7. pp. 570-573.

Brunner, R. and Aissaoui, H. and Boss, C. and Bozdech, Z. and Brun, R. and Corminboeuf, O. and Delahaye, S. and Fischli, C. and Heidmann, B. and Kaiser, M. and Kamber, J. and Meyer, S. and Papastogiannidis, P. and Siegrist, R. and Voss, Till S. and Welford, R. and Wittlin, S. and Binkert, C.. (2012) Identification of a new chemical class of antimalarials. Journal of infectious diseases, Vol. 206, no. 5. pp. 735-743.

Wittlin, S. and Ekland, E. and Craft, J. C. and Lotharius, J. and Bathurst, I. and Fidock, D. A. and Fernandes, P.. (2012) In vitro and in vivo activity of Solithromycin (CEM-101) against Plasmodium species. Antimicrobial agents and chemotherapy : AAC, Vol. 56, H. 2. pp. 703-707.

Wenzler, T. and Steinhuber, A. and Wittlin, S. and Scheurer, C. and Brun, R. and Trampuz, A.. (2012) Isothermal microcalorimetry, a new tool to monitor drug action against Trypanosoma brucei and Plasmodium falciparum. PLoS neglected tropical diseases, Vol. 6, H. 6 , e1668.

Dreyer, A. M. and Matile, H. and Papastogiannidis, P. and Kamber, J. and Favuzza, P. and Voss, Till S. and Wittlin, S. and Pluschke, G.. (2012) Passive immunoprotection of Plasmodium falciparum-infected mice designates the CyRPA as candidate malaria vaccine antigen. Journal of immunology : official journal of the American Association of Immunologists, Vol. 188, H. 12. pp. 6225-6237.

Li, Y. and Hao, H. D. and Wittlin, S. and Wu, Y.. (2012) Simple analogues of Qinghaosu (Artemisinin). Chemistry : an Asian journal / an ACES journal, Vol. 7, H. 8. pp. 1881-1886.

González, Cabrera and Douelle, F. and Younis, Y. E. and Feng, T. S. and Lemanach, C. and Nchinda, A. T. and Street, L. J. and Scheurer, C. and Kamber, J. and White, K. L. and Montagnat, O. D. and Ryan, E. and Katneni, K. and Zabiulla, K. M. and Joseph, J. T. and Bashyam, S. and Waterson, D. and Witty, M. J. and Charman, S. A. and Wittlin, S. and Chibale, K.. (2012) Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines. Journal of medicinal chemistry, 55 (24). pp. 11022-11030.

Delves, M. and Plouffe, D. and Scheurer, C. and Meister, S. and Wittlin, S. and Winzeler, E. A. and Sinden, R. E. and Leroy, D.. (2012) The activities of current antimalarial drugs on the life cycle stages of Plasmodium : a comparative study with human and rodent parasites. PLoS medicine, Vol. 9, H. 2 , e1001169.

2011

Schiaffo, C. E. and Rottmann, M. and Wittlin, S. and Dussault, P. H.. (2011) 3-alkoxy-1,2-dioxolanes : synthesis and evaluation as potential antimalarial agents. ACS medicinal chemistry letters, Vol. 2, H. 4. pp. 316-319.

Barker, R. H. Jr. and Urgaonkar, S. and Mazitschek, R. and Celatka, C. and Skerlj, R. and Cortese, J. F. and Tyndall, E. and Liu, H. and Cromwell, M. and Sidhu, A. B. and Guerrero-Bravo, J. E. and Crespo-Llado, K. N. and Serrano, A. E. and Lin, J. W. and Janse, C. J. and Khan, S. M. and Duraisingh, M. and Coleman, B. I. and Angulo-Barturen, I. and Jimenez-Diaz, M. B. and Magan, N. and Gomez, V. and Ferrer, S. and Martinez, M. S. and Wittlin, S. and Papastogiannidis, P. and O'Shea, T. and Klinger, J. D. and Bree, M. and Lee, E. and Levine, M. and Wiegand, R. C. and Munoz, B. and Wirth, D. F. and Clardy, J. and Bathurst, I. and Sybertz, E.. (2011) Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum. Antimicrobial agents and chemotherapy, 55 (6). pp. 2612-2622.

Chadwick, J. and Amewu, R. K. and Marti, F. and Bousejra-El Garah F., and Sharma, R. and Berry, N. G. and Stocks, P. A. and Burrell-Saward H., and Wittlin, S. and Rottmann, M. and Brun, R. and Taramelli, D. and Parapini, S. and Ward, S. A. and O'Neill P. M., . (2011) Antimalarial mannoxanes : hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action. ChemMedChem : chemistry enabling drug discovery, Vol. 6, H. 8. pp. 1357-1361.

González Cabrera D., and Douelle, F. and Feng, T. S. and Nchinda, A. T. and Younis, Y. and White, K. L. and Wu, Q. and Ryan, E. and Burrows, J. N. and Waterson, D. and Witty, M. J. and Wittlin, S. and Charman, S. A. and Chibale, K.. (2011) Novel orally active antimalarial thiazoles. Journal of medicinal chemistry, 54 (21). pp. 7713-7719.

Skerlj, R. T. and Bastos, C. M. and Booker, M. L. and Kramer, M. L. and Barker, R. H. and Celatka, C. A. and O'Shea T. J., and Munoz, B. and Sidhu, A. B. and Cortese, J. F. and Wittlin, S. and Papastogiannidis, P. and Angulo-Barturen I., and Jimenez-Diaz M. B., and Sybertz, E.. (2011) Optimization of potent inhibitors of P. falciparum dihydroorotate dehydrogenase for the treatment of malaria. ACS medicinal chemistry letters, Vol. 2, H. 9. pp. 708-713.

Vargas, S. and Ndjoko Ioset K., and Hay, A. E. and Ioset, J. R. and Wittlin, S. and Hostettmann, K.. (2011) Screening medicinal plants for the detection of novel antimalarial products applying the inhibition of beta-hematin formation. Journal of pharmaceutical and biomedical analysis, Vol. 56, H. 5. pp. 880-886.

Shi, X. L. and Ge, J. F. and Liu, B. Q. and Kaiser, M. and Wittlin, S. and Brun, R. and Ihara, M.. (2011) Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives. Bioorganic & medicinal chemistry letters : a Tetrahedron publication for the rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Vol. 21, H. 19. pp. 5804-5807.

Lu, Y. T. and Arai, C. and Ge, J. F. and Ren, W. S. and Kaiser, M. and Wittlin, S. and Brun, R. and Lu, J. M. and Ihara, M.. (2011) Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive phenothiazinium chlorides. Dyes and pigments : an international journal, Vol. 89, H. 1. pp. 44-48.

Charman, S. A. and Arbe-Barnes S., and Bathurst, I. C. and Brun, R. and Campbell, M. and Charman, W. N. and Chiu, F. C. and Chollet, J. and Craft, J. C. and Creek, D. J. and Dong, Y. and Matile, H. and Maurer, M. and Morizzi, J. and Nguyen, T. and Papastogiannidis, P. and Scheurer, C. and Shackleford, D. M. and Sriraghavan, K. and Stingelin, L. and Tang, Y. and Urwyler, H. and Wang, X. and White, K. L. and Wittlin, S. and Zhou, L. and Vennerstrom, J. L.. (2011) Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proceedings of the National Academy of Sciences of the United States of America, Vol. 108, H. 11. pp. 4400-4405.

2010

Wright, C. W. and Linley, P. A. and Brun, R. and Wittlin, S. and Hsu, E.. (2010) Ancient Chinese methods are remarkably effective for the preparation of artemisinin-rich extracts of Qing Hao with potent antimalarial activity. Molecules, Vol. 15, H. 2. pp. 804-812.

Abiodun, O. O. and Gbotosho, G. O. and Ajaiyeoba, E. O. and Happi, C. T. and Hofer, S. and Wittlin, S. and Sowunmi, A. and Brun, R. and Oduola, A. M. J.. (2010) Comparison of SYBR Green I-, PicoGreen-, and [H-3]-hypoxanthine-based assays for in vitro antimalarial screening of plants from Nigerian ethnomedicine. Parasitology research : Organ der Deutschen Gesellschaft für Parasitologie, Vol. 106, H. 4. pp. 933-939.

Ge, J. F. and Arai, C. and Yang, M. and Bakar, M. A. and Lu, J. and Ismail, N. S. M. and Wittlin, S. and Kaiser, M. and Brun, R. and Charman, S. A. and Nguyen, T. and Morizzi, J. and Itoh, I. and Ihara, M.. (2010) Discovery of novel benzo[a]phenoxazine SSJ-183 as a drug candidate for malaria. ACS medicinal chemistry letters, Vol. 1, H. 7. pp. 360-364.

O'Neill P. M., and Amewu, R. K. and Nixon, G. L. and Bousejra, E. F. and Mungthin, M. and Chadwick, J. and Shone, A. E. and Vivas, L. and Lander, H. and Barton, V. and Muangnoicharoen, S. and Bray, P. G. and Davies, J. and Park, B. K. and Wittlin, S. and Brun, R. and Preschel, M. and Zhang, K. and Ward, S. A.. (2010) Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins. Angewandte Chemie. International edition in English, Vol. 49, H. 33. pp. 5693-5697.

Booker, M. L. and Bastos, C. M. and Kramer, M. L. and Barker, R. H. and Skerlj, R. and Sidhu, A. B. and Deng, X. and Celatka, C. and Cortese, J. F. and Guerrero Bravo J. E., and Crespo Llado K. N., and Serrano, A. E. and Angulo-Barturen I., and Jimenez-Diaz M. B., and Viera, S. and Garuti, H. and Wittlin, S. and Papastogiannidis, P. and Lin, J. W. and Janse, C. J. and Khan, S. M. and Duraisingh, M. and Coleman, B. and Goldsmith, E. J. and Phillips, M. A. and Munoz, B. and Wirth, D. F. and Klinger, J. D. and Wiegand, R. and Sybertz, E.. (2010) Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model. Journal of Biological Chemistry, Vol. 285, H. 43. pp. 33054-33064.

Nzila, A. and Rottmann, M. and Chitnumsub, P. and Kiara, S. M. and Kamchonwongpaisan, S. and Maneeruttanarungroj, C. and Taweechai, S. and Yeung, B. K. and Goh, A. and Lakshminarayana, S. B. and Zou, B. and Wong, J. and Ma, N. L. and Weaver, M. and Keller, T. H. and Dartois, V. and Wittlin, S. and Brun, R. and Yuthavong, Y. and Diagana, T. T.. (2010) Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. Antimicrobial agents and chemotherapy : AAC, Vol. 54, H. 6. pp. 2603-2610.

Burgess, S. J. and Kelly, J. X. and Shomloo, S. and Wittlin, S. and Brun, R. and Liebmann, K. and Peyton, D. H.. (2010) Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. Journal of medicinal chemistry, 53 (17). pp. 6477-6489.

Tang, Y. and Wittlin, S. and Charman, S. A. and Chollet, J. and Chiu, F. C. and Morizzi, J. and Johnson, L. M. and Tomas, J. S. and Scheurer, C. and Snyder, C. and Zhou, L. and Dong, Y. and Charman, W. N. and Matile, H. and Urwyler, H. and Dorn, A. and Vennerstrom, J. L.. (2010) The comparative antimalarial properties of weak base and neutral synthetic ozonides. Bioorganic and Medicinal Chemistry Letters, Vol. 20, H. 2. pp. 563-566.

Dong, Y. and McCullough, K. J. and Wittlin, S. and Chollet, J. and Vennerstrom, J. L.. (2010) The structure and antimalarial activity of dispiro-1,2,4,5-tetraoxanes derived from (+)-dihydrocarvone. Bioorganic and Medicinal Chemistry Letters, Vol. 20, H. 22. pp. 6359-6361.

Dong, Y. and Wittlin, S. and Sriraghavan, K. and Chollet, J. and Charman, S. A. and Charman, W. N. and Scheurer, C. and Urwyler, H. and Santo, T. J. and Snyder, C. and Creek, D. J. and Morizzi, J. and Koltun, M. and Matile, H. and Wang, X. and Padmanilayam, M. and Tang, Y. and Dorn, A. and Brun, R. and Vennerstrom, J. L.. (2010) The structure-activity relationship of the antimalarial ozonide arterolane (OZ277). Journal of Medicinal Chemistry, 53 (1). pp. 481-491.

2009

Tritten, L. and Matile, H. and Brun, R. and Wittlin, S.. (2009) A new double-antibody sandwich ELISA targeting Plasmodium falciparum aldolase to evaluate anti-malarial drug sensitivity. Malaria Journal, Vol. 8 , 226.

Sturm, N. and Hu, Y. and Zimmermann, H. and Fritz-Wolf K., and Wittlin, S. and Rahlfs, S. and Becker, K.. (2009) Compounds structurally related to ellagic acid show improved antiplasmodial activity. Antimicrobial agents and chemotherapy : AAC, Vol. 53, H. 2. pp. 622-630.

Kelly, J. X. and Smilkstein, M. J. and Brun, R. and Wittlin, S. and Cooper, R. A. and Lane, K. D. and Janowsky, A. and Johnson, R. A. and Dodean, R. A. and Winter, R. and Hinrichs, D. J. and Riscoe, M. K.. (2009) Discovery of dual function acridones as a new antimalarial chemotype. Nature, Vol. 459, H. 7244. pp. 270-273.

Irungu, B. and Kiboi, D. and Langat, B. and Rukunga, G. and Wittlin, S. and Nzila, A.. (2009) Methotrexate and aminopterin lack in vivo antimalarial activity against murine malaria species. Experimental parasitology : EP, Vol. 123, H. 2. pp. 118-121.

Efange, S. M. and Brun, R. and Wittlin, S. and Connolly, J. D. and Hoye, T. R. and McAkam, T. and Makolo, F. L. and Mbah, J. A. and Nelson, D. P. and Nyongbela, K. D. and Wirmum, C. K.. (2009) Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity. Journal of Natural Products, Vol. 72, H. 2. pp. 280-283.

Kiboi, D. M. and Irungu, B. N. and Langat, B. and Wittlin, S. and Brun, R. and Chollet, J. and Abiodun, O. and Nganga, J. K. and Nyambati, V. C. and Rukunga, G. M. and Bell, A. and Nzila, A.. (2009) Plasmodium berghei ANKA: selection of resistance to piperaquine and lumefantrine in a mouse model. Experimental parasitology : EP, Vol. 122, H. 3. pp. 196-202.

Wang, X. and Creek, D. J. and Schiaffo, C. E. and Dong, Y. and Chollet, J. and Scheurer, C. and Wittlin, S. and Charman, S. A. and Dussault, P. H. and Wood, J. K. and Vennerstrom, J. L.. (2009) Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs : relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity. Bioorganic & medicinal chemistry letters : a Tetrahedron publication for the rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Vol. 19, H. 16. pp. 4542-4545.

Pudhom, K. and Ge, M. F. and Arai, C. and Yang, M. and Kaiser, M. and Wittlin, S. and Brun, R. and Itoh, I. and Ihara, M.. (2009) Synthesis and biological properties of a rhodacyanine derivative, Ssj-127, having high efficacy against malaria protozoa. Heterocycles : an international journal for reviews and communications in heterocyclic chemistry, Vol. 77, H. 1. pp. 207-210.

2008

Li, J. V. and Wang, Y. and Saric, J. and Nicholson, J. K. and Dirnhofer, S. and Singer, B. H. and Tanner, M. and Wittlin, S. and Holmes, E. and Utzinger, J.. (2008) Global metabolic responses of NMRI mice to an experimental Plasmodium berghei infection. Journal of Proteome Research, Vol. 7, H. 9. pp. 3948-3956.