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Items where Author is "Wittlin, Sergio"

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Number of items: 58.

2020

Burgert, Lydia and Rottmann, Matthias and Wittlin, Sergio and Gobeau, Nathalie and Krause, Andreas and Dingemanse, Jasper and Möhrle, Jörg J. and Penny, Melissa A.. (2020) Ensemble modeling highlights importance of understanding parasite-host behavior in preclinical antimalarial drug development. Scientific reports, 10. p. 4410.

Kokkonda, Sreekanth and Deng, Xiaoyi and White, Karen L. and El Mazouni, Farah and White, John and Shackleford, David M. and Katneni, Kasiram and Chiu, Francis C. K. and Barker, Helena and McLaren, Jenna and Crighton, Elly and Chen, Gong and Angulo-Barturen, Inigo and Jimenez-Diaz, Maria Belen and Ferrer, Santiago and Huertas-Valentin, Leticia and Martinez-Martinez, Maria Santos and Lafuente-Monasterio, Maria Jose and Chittimalla, Rajesh and Shahi, Shatrughan P. and Wittlin, Sergio and Waterson, David and Burrows, Jeremy N. and Matthews, Dave and Tomchick, Diana and Rathod, Pradipsinh K. and Palmer, Michael J. and Charman, Susan A. and Phillips, Margaret A.. (2020) Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of malaria. Journal of medicinal chemistry, 63 (9). pp. 4929-4956.

2019

Schalkwijk, Joost and Allman, Erik L. and Jansen, Patrick A. M. and de Vries, Laura E. and Verhoef, Julie M. J. and Jackowski, Suzanne and Botman, Peter N. M. and Beuckens-Schortinghuis, Christien A. and Koolen, Karin M. J. and Bolscher, Judith M. and Vos, Martijn W. and Miller, Karen and Reeves, Stacy A. and Pett, Helmi and Trevitt, Graham and Wittlin, Sergio and Scheurer, Christian and Sax, Sibylle and Fischli, Christoph and Angulo-Barturen, Iñigo and Jiménez-Diaz, Mariá Belén and Josling, Gabrielle and Kooij, Taco W. A. and Bonnert, Roger and Campo, Brice and Blaauw, Richard H. and Rutjes, Floris P. J. T. and Sauerwein, Robert W. and Llinás, Manuel and Hermkens, Pedro H. H. and Dechering, Koen J.. (2019) Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum. Science Translational Medicine, 11 (510). eaas9917.

Okombo, John and Brunschwig, Christel and Singh, Kawaljit and Dziwornu, Godwin Akpeko and Barnard, Linley and Njoroge, Mathew and Wittlin, Sergio and Chibale, Kelly. (2019) Antimalarial pyrido[1,2-a]benzimidazole derivatives with mannich base side chains: synthesis, pharmacological evaluation and reactive metabolite trapping studies. ACS infectious diseases, 5 (3). pp. 372-384.

Gilson, Paul R. and Nguyen, William and Poole, William A. and Teixeira, Jose E. and Thompson, Jennifer K. and Guo, Kaiyuan and Stewart, Rebecca J. and Ashton, Trent D. and White, Karen L. and Sanz, Laura M. and Gamo, Francisco-Javier and Charman, Susan A. and Wittlin, Sergio and Duffy, James and Tonkin, Christopher J. and Tham, Wai-Hong and Crabb, Brendan S. and Cooke, Brian M. and Huston, Christopher D. and Cowman, Alan F. and Sleebs, Brad E.. (2019) Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Evaluation of 4-amino 2-anilinoquinazolines against Plasmodium and other apicomplexan parasites in vitro and in a P. falciparum humanized NOD-scid IL2Rynull mouse model of malaria. Antimicrobial agents and chemotherapy, 63 (3). e01804-18.

Baragaña, Beatriz and Forte, Barbara and Choi, Ryan and Nakazawa Hewitt, Stephen and Bueren-Calabuig, Juan A. and Pisco, João Pedro and Peet, Caroline and Dranow, David M. and Robinson, David A. and Jansen, Chimed and Norcross, Neil R. and Vinayak, Sumiti and Anderson, Mark and Brooks, Carrie F. and Cooper, Caitlin A. and Damerow, Sebastian and Delves, Michael and Dowers, Karen and Duffy, James and Edwards, Thomas E. and Hallyburton, Irene and Horst, Benjamin G. and Hulverson, Matthew A. and Ferguson, Liam and Jiménez-Díaz, María Belén and Jumani, Rajiv S. and Lorimer, Donald D. and Love, Melissa S. and Maher, Steven and Matthews, Holly and McNamara, Case W. and Miller, Peter and O'Neill, Sandra and Ojo, Kayode K. and Osuna-Cabello, Maria and Pinto, Erika and Post, John and Riley, Jennifer and Rottmann, Matthias and Sanz, Laura M. and Scullion, Paul and Sharma, Arvind and Shepherd, Sharon M. and Shishikura, Yoko and Simeons, Frederick R. C. and Stebbins, Erin E. and Stojanovski, Laste and Straschil, Ursula and Tamaki, Fabio K. and Tamjar, Jevgenia and Torrie, Leah S. and Vantaux, Amélie and Witkowski, Benoît and Wittlin, Sergio and Yogavel, Manickam and Zuccotto, Fabio and Angulo-Barturen, Iñigo and Sinden, Robert and Baum, Jake and Gamo, Francisco-Javier and Mäser, Pascal and Kyle, Dennis E. and Winzeler, Elizabeth A. and Myler, Peter J. and Wyatt, Paul G. and Floyd, David and Matthews, David and Sharma, Amit and Striepen, Boris and Huston, Christopher D. and Gray, David W. and Fairlamb, Alan H. and Pisliakov, Andrei V. and Walpole, Chris and Read, Kevin D. and Van Voorhis, Wesley C. and Gilbert, Ian H.. (2019) Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proceedings of the National Academy of Sciences of the United States of America, 116 (14). pp. 7015-7020.

Kumar, Malkeet and Okombo, John and Mambwe, Dickson and Taylor, Dale and Lawrence, Nina and Reader, Janette and van der Watt, Mariëtte and Fontinha, Diana and Sanches-Vaz, Margarida and Bezuidenhout, Belinda C. and Lauterbach, Sonja B. and Liebenberg, Dale and Birkholtz, Lyn-Marie and Coetzer, Theresa L. and Prudêncio, Miguel and Egan, Timothy J. and Wittlin, Sergio and Chibale, Kelly. (2019) Multistage antiplasmodium activity of astemizole analogues and inhibition of hemozoin formation as a contributor to their mode of action. ACS infectious diseases, 5 (2). pp. 303-315.

Jourdan, Joëlle and Walz, Annabelle and Matile, Hugues and Schmidt, Alexander and Wu, Jianbo and Wang, Xiaofang and Dong, Yuxiang and Vennerstrom, Jonathan L. and Schmidt, Remo S. and Wittlin, Sergio and Mäser, Pascal. (2019) Stochastic Protein Alkylation by Antimalarial Peroxides. ACS infectious diseases, 5 (12). pp. 2067-2075.

Jourdan, Joëlle and Walz, Annabelle and Matile, Hugues and Schmidt, Alexander and Wu, Jianbo and Wang, Xiaofang and Dong, Yuxiang and Vennerstrom, Jonathan L. and Schmidt, Remo S. and Wittlin, Sergio and Mäser, Pascal. (2019) Stochastic protein alkylation by antimalarial peroxides. ACS infectious diseases, 5 (12). pp. 2067-2075.

Mayoka, Godfrey and Njoroge, Mathew and Okombo, John and Gibhard, Liezl and Sanches-Vaz, Margarida and Fontinha, Diana and Birkholtz, Lyn-Marie and Reader, Janette and van der Watt, Mariëtte and Coetzer, Theresa L. and Lauterbach, Sonja and Churchyard, Alisje and Bezuidenhout, Belinda and Egan, Timothy J. and Yeates, Clive Leonard and Wittlin, Sergio and Prudêncio, Miguel and Chibale, Kelly. (2019) Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria. Journal of medicinal chemistry, 62 (2). pp. 1022-1035.

2018

Kaur, Gurminder and Pavadai, Elumalai and Wittlin, Sergio and Chibale, Kelly. (2018) 3D-QSAR modeling and synthesis of new fusidic acid derivatives as antiplasmodial agents. Journal of Chemical Information and Modeling, 58 (8). pp. 1553-1560.

Le Manach, Claire and Paquet, Tanya and Wicht, Kathryn and Nchinda, Aloysius T. and Brunschwig, Christel and Njoroge, Mathew and Gibhard, Liezl and Taylor, Dale and Lawrence, Nina and Wittlin, Sergio and Eyermann, Charles J. and Basarab, Gregory S. and Duffy, James and Fish, Paul V. and Street, Leslie J. and Chibale, Kelly. (2018) Antimalarial lead-optimization studies on a 2,6-imidazopyridine series within a constrained chemical space to circumvent atypical dose-response curves against multidrug resistant parasite strains. Journal of medicinal chemistry, 61 (20). pp. 9371-9385.

Grogg, Marcel and Hilvert, Donald and Ebert, Marc-Olivier and Beck, Albert K. and Seebach, Dieter and Kurth, Felix and Dittrich, Petra S. and Sparr, Christof and Wittlin, Sergio and Rottmann, Matthias and Mäser, Pascal. (2018) Cell penetration, herbicidal activity, and in-vivo-toxicity of oligo-arginine derivatives and of novel guanidinium-rich compounds derived from the biopolymer cyanophycin. Helvetica Chimica Acta, 101 (10). e1800112.

Nchinda, Aloysius T. and Le Manach, Claire and Paquet, Tanya and Gonzàlez Cabrera, Diego and Wicht, Kathryn J. and Brunschwig, Christel and Njoroge, Mathew and Abay, Efrem and Taylor, Dale and Lawrence, Nina and Wittlin, Sergio and Jiménez-Díaz, María-Belén and Santos Martínez, María and Ferrer, Santiago and Angulo-Barturen, Iñigo and Lafuente-Monasterio, Maria Jose and Duffy, James and Burrows, Jeremy and Street, Leslie J. and Chibale, Kelly. (2018) Identification of fast-acting 2,6-disubstituted imidazopyridines that are efficacious in the In Vivo humanized Plasmodium falciparum nodscidil2rgamma (null) mouse model of malaria. Journal of medicinal chemistry, 61 (9). pp. 4213-4227.

Gibhard, Liezl and Njoroge, Mathew and Paquet, Tanya and Brunschwig, Christel and Taylor, Dale and Lawrence, Nina and Abay, Efrem and Wittlin, Sergio and Wiesner, Lubbe and Street, Leslie J. and Chibale, Kelly and Basarab, Gregory S.. (2018) Investigating sulfoxide to sulfone conversion as a prodrug strategy for a PI4K inhibitor in a humanized mouse model of malaria. Antimicrobial agents and chemotherapy, 62 (12). e00261-18.

Brunschwig, Christel and Lawrence, Nina and Taylor, Dale and Abay, Efrem and Njoroge, Mathew and Basarab, Gregory S. and Le Manach, Claire and Paquet, Tanya and Cabrera, Diego Gonzàlez and Nchinda, Aloysius T. and de Kock, Carmen and Wiesner, Lubbe and Denti, Paolo and Waterson, David and Blasco, Benjamin and Leroy, Didier and Witty, Michael J. and Donini, Cristina and Duffy, James and Wittlin, Sergio and White, Karen L. and Charman, Susan A. and Jiménez-Díaz, Maria Belén and Angulo-Barturen, Iñigo and Herreros, Esperanza and Gamo, Francisco Javier and Rochford, Rosemary and Mancama, Dalu and Coetzer, Theresa L. and van der Watt, Mariëtte E. and Reader, Janette and Birkholtz, Lyn-Marie and Marsh, Kennan C. and Solapure, Suresh M. and Burke, John E. and McPhail, Jacob A. and Vanaerschot, Manu and Fidock, David A. and Fish, Paul V. and Siegl, Peter and Smith, Dennis A. and Wirjanata, Grennady and Noviyanti, Rintis and Price, Ric N. and Marfurt, Jutta and Silue, Kigbafori D. and Street, Leslie J. and Chibale, Kelly. (2018) UCT943, a next generation Plasmodium falciparum PI4K inhibitor preclinical candidate for the treatment of malaria. Antimicrobial agents and chemotherapy, 62 (9). e00012-e00018.

2017

Leven, Michael and Knaab, Tanja C. and Held, Jana and Duffy, Sandra and Meister, Stephan and Fischli, Christoph and Meitzner, Diane and Lehmann, Ursula and Lungerich, Beate and Kuna, Krystina and Stahlke, Petra and Delves, Michael J. and Buchholz, Mirko and Winzeler, Elizabeth A. and Avery, Vicky M. and Mordmüller, Benjamin and Wittlin, Sergio and Kurz, Thomas. (2017) 3-hydroxy-N'-arylidenepropanehydrazonamides with halo-substituted phenanthrene scaffolds cure P. berghei infected mice when administered perorally. Journal of Medicinal Chemistry, 60 (14). pp. 6036-6044.

Paquet, Tanya and Le Manach, Claire and Cabrera, Diego González and Younis, Yassir and Henrich, Philipp P. and Abraham, Tara S. and Lee, Marcus C. S. and Basak, Rajshekhar and Ghidelli-Disse, Sonja and Lafuente-Monasterio, María José and Bantscheff, Marcus and Ruecker, Andrea and Blagborough, Andrew M. and Zakutansky, Sara E. and Zeeman, Anne-Marie and White, Karen L. and Shackleford, David M. and Mannila, Janne and Morizzi, Julia and Scheurer, Christian and Angulo-Barturen, Iñigo and Martínez, María Santos and Ferrer, Santiago and Sanz, Laura María and Gamo, Francisco Javier and Reader, Janette and Botha, Mariette and Dechering, Koen J. and Sauerwein, Robert W. and Tungtaeng, Anchalee and Vanachayangkul, Pattaraporn and Lim, Chek Shik and Burrows, Jeremy and Witty, Michael J. and Marsh, Kennan C. and Bodenreider, Christophe and Rochford, Rosemary and Solapure, Suresh M. and Jiménez-Díaz, María Belén and Wittlin, Sergio and Charman, Susan A. and Donini, Cristina and Campo, Brice and Birkholtz, Lyn-Marie and Hanson, Kirsten K. and Drewes, Gerard and Kocken, Clemens H. M. and Delves, Michael J. and Leroy, Didier and Fidock, David A. and Waterson, David and Street, Leslie J. and Chibale, Kelly. (2017) Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase. Science translational medicine, 9 (387). eaad9735.

Singh, Kawaljit and Okombo, John and Brunschwig, Christel and Ndubi, Ferdinand and Barnard, Linley and Wilkinson, Chad and Njogu, Peter M. and Njoroge, Mathew and Laing, Lizahn and Machado, Marta and Prudêncio, Miguel and Reader, Janette and Botha, Mariette and Nondaba, Sindisiwe and Birkholtz, Lyn-Marie and Lauterbach, Sonja and Churchyard, Alisje and Coetzer, Theresa L. and Burrows, Jeremy N. and Yeates, Clive and Denti, Paolo and Wiesner, Lubbe and Egan, Timothy J. and Wittlin, Sergio and Chibale, Kelly. (2017) Antimalarial pyrido[1,2-a]benzimidazoles : lead optimization, parasite life cycle stage profile, mechanistic evaluation, killing kinetics, and in vivo oral efficacy in a mouse model. Journal of medicinal chemistry, 60 (4). pp. 1432-1448.

Krieg, Reimar and Jortzik, Esther and Goetz, Alice-Anne and Blandin, Stéphanie and Wittlin, Sergio and Elhabiri, Mourad and Rahbari, Mahsa and Nuryyeva, Selbi and Voigt, Kerstin and Dahse, Hans-Martin and Brakhage, Axel and Beckmann, Svenja and Quack, Thomas and Grevelding, Christoph G. and Pinkerton, Anthony B. and Schönecker, Bruno and Burrows, Jeremy and Davioud-Charvet, Elisabeth and Rahlfs, Stefan and Becker, Katja. (2017) Arylmethylamino steroids as antiparasitic agents. Nature communications, 8. p. 14478.

Baumgärtner, Fabian and Jourdan, Joëlle and Scheurer, Christian and Blasco, Benjamin and Campo, Brice and Mäser, Pascal and Wittlin, Sergio. (2017) In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate. Malaria journal, 16. p. 45.

Abla, Nada and Bashyam, Sridevi and Charman, Susan A. and Greco, Béatrice and Hewitt, Philip and Jiménez-Díaz, Maria Belén and Katneni, Kasiram and Kubas, Holger and Picard, Didier and Sambandan, Yuvaraj and Sanz, Laura and Smith, Dennis and Wang, Tai and Willis, Paul and Wittlin, Sergio and Spangenberg, Thomas. (2017) Long-lasting and fast-acting in vivo efficacious antiplasmodial azepanylcarbazole amino alcohol. ACS medicinal chemistry letters, 8 (12). pp. 1304-1308.

Xu, Ze-Jun and Wittlin, Sergio and Wu, Yikang. (2017) Probing the peroxycarbenium [3+2] cycloaddition reactions with 1,2-disubstituted ethylenes: results and insights. Chemistry (Weinheim an der Bergstrasse, Germany), 23 (9). pp. 2031-2034.

Dong, Yuxiang and Wang, Xiaofang and Kamaraj, Sriraghavan and Bulbule, Vivek J. and Chiu, Francis C. K. and Chollet, Jacques and Dhanasekaran, Manickam and Hein, Christopher D. and Papastogiannidis, Petros and Morizzi, Julia and Shackleford, David M. and Barker, Helena and Ryan, Eileen and Scheurer, Christian and Tang, Yuanqing and Zhao, Qingjie and Zhou, Lin and White, Karen L. and Urwyler, Heinrich and Charman, William N. and Matile, Hugues and Wittlin, Sergio and Charman, Susan A. and Vennerstrom, Jonathan L.. (2017) Structure-activity relationship of the antimalarial ozonide artefenomel (OZ439). Journal of medicinal chemistry, 60 (7). pp. 2654-2668.

Espinoza-Moraga, Marlene and Singh, Kawaljit and Njoroge, Mathew and Kaur, Gurminder and Okombo, John and De Kock, Carmen and Smith, Peter J. and Wittlin, Sergio and Chibale, Kelly. (2017) Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents. Bioorganic & medicinal chemistry, 27 (3). pp. 658-661.

2016

Ng, Caroline L. and Siciliano, Giulia and Lee, Marcus C. S. and de Almeida, Mariana J. and Corey, Victoria C. and Bopp, Selina E. and Bertuccini, Lucia and Wittlin, Sergio and Kasdin, Rachel G. and Le Bihan, Amélie and Clozel, Martine and Winzeler, Elizabeth A. and Alano, Pietro and Fidock, David A.. (2016) CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs. Molecular microbiology, 101 (3). pp. 381-393.

Le Bihan, Amélie and de Kanter, Ruben and Angulo-Barturen, Iñigo and Binkert, Christoph and Boss, Christoph and Brun, Reto and Brunner, Ralf and Buchmann, Stephan and Burrows, Jeremy and Dechering, Koen J. and Delves, Michael and Ewerling, Sonja and Ferrer, Santiago and Fischli, Christoph and Gamo-Benito, Francisco Javier and Gnädig, Nina F. and Heidmann, Bibia and Jiménez-Díaz, María Belén and Leroy, Didier and Martínez, Maria Santos and Meyer, Solange and Moehrle, Joerg J. and Ng, Caroline L. and Noviyanti, Rintis and Ruecker, Andrea and Sanz, Laura María and Sauerwein, Robert W. and Scheurer, Christian and Schleiferboeck, Sarah and Sinden, Robert and Snyder, Christopher and Straimer, Judith and Wirjanata, Grennady and Marfurt, Jutta and Price, Ric N. and Weller, Thomas and Fischli, Walter and Fidock, David A. and Clozel, Martine and Wittlin, Sergio. (2016) Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling. PLoS medicine, 13 (10). e1002138.

Boss, Christoph and Aissaoui, Hamed and Amaral, Nathalie and Bauer, Aude and Bazire, Stephanie and Binkert, Christoph and Brun, Reto and Bürki, Cédric and Ciana, Claire-Lise and Corminboeuf, Olivier and Delahaye, Stephane and Dollinger, Claire and Fischli, Christoph and Fischli, Walter and Flock, Alexandre and Frantz, Marie-Céline and Girault, Malory and Grisostomi, Corinna and Friedli, Astrid and Heidmann, Bibia and Hinder, Claire and Jacob, Gael and Le Bihan, Amelie and Malrieu, Sophie and Mamzed, Saskia and Merot, Aurelien and Meyer, Solange and Peixoto, Sabrina and Petit, Nolwenn and Siegrist, Romain and Trollux, Julien and Weller, Thomas and Wittlin, Sergio. (2016) Discovery and characterization of ACT-451840 : an antimalarial drug with a novel mechanism of action. ChemMedChem, 11 (18). pp. 1995-2014.

Baragaña, Beatriz and Norcross, Neil R. and Wilson, Caroline and Porzelle, Achim and Hallyburton, Irene and Grimaldi, Raffaella and Osuna-Cabello, Maria and Norval, Suzanne and Riley, Jennifer and Stojanovski, Laste and Simeons, Frederick R. C. and Wyatt, Paul G. and Delves, Michael J. and Meister, Stephan and Duffy, Sandra and Avery, Vicky M. and Winzeler, Elizabeth A. and Sinden, Robert E. and Wittlin, Sergio and Frearson, Julie A. and Gray, David W. and Fairlamb, Alan H. and Waterson, David and Campbell, Simon F. and Willis, Paul and Read, Kevin D. and Gilbert, Ian H.. (2016) Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy. Journal of medicinal chemistry, 59 (21). pp. 9672-9685.

Le Manach, Claire and Nchinda, Aloysius T. and Paquet, Tanya and Gonzàlez Cabrera, Diego and Younis, Yassir and Han, Ze and Bashyam, Sridevi and Zabiulla, Mohammed and Taylor, Dale and Lawrence, Nina and White, Karen L. and Charman, Susan A. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Botha, Mariëtte E. and Nondaba, Sindisiswe H. and Reader, Janette and Birkholtz, Lyn-Marie and Jiménez-Díaz, María Belén and Martínez, María Santos and Ferrer, Santiago and Angulo-Barturen, Iñigo and Meister, Stephan and Antonova-Koch, Yevgeniya and Winzeler, Elizabeth A. and Street, Leslie J. and Chibale, Kelly. (2016) Identification of a potential antimalarial drug candidate from a series of 2-aminopyrazines by optimization of aqueous solubility and potency across the parasite life cycle. Journal of medicinal chemistry, 59 (21). pp. 9890-9905.

Pavadai, Elumalai and El Mazouni, Farah and Wittlin, Sergio and de Kock, Carmen and Phillips, Margaret A. and Chibale, Kelly. (2016) Identification of new human malaria parasite Plasmodium falciparum dihydroorotate dehydrogenase inhibitors by pharmacophore and structure-based virtual screening. Journal of chemical information and modeling, 56 (3). pp. 548-562.

Jourdan, Joëlle and Hugues, Matile and Reift, Ellen and Biehlmaier, Oliver and Dong, Yuxiang and Wang, Xiaofang and Mäser, Pascal and Vennerstrom, Jonathan and Wittlin, Sergio. (2016) Monoclonal antibodies that recognize the alkylation signature of antimalarial ozonides OZ277 (Arterolane) and OZ439 ( Artefenomel). ACS infectious diseases, 2 (1). pp. 54-61.

Williamson, Alice E. and Ylioja, Paul M. and Robertson, Murray N. and Antonova-Koch, Yevgeniya and Avery, Vicky and Baell, Jonathan B. and Batchu, Harikrishna and Batra, Sanjay and Burrows, Jeremy N. and Bhattacharyya, Soumya and Calderon, Felix and Charman, Susan A. and Clark, Julie and Crespo, Benigno and Dean, Matin and Debbert, Stefan L. and Delves, Michael and Dennis, Adelaide S. M. and Deroose, Frederik and Duffy, Sandra and Fletcher, Sabine and Giaever, Guri and Hallyburton, Irene and Gamo, Francisco-Javier and Gebbia, Marinella and Guy, R. Kiplin and Hungerford, Zoe and Kirk, Kiaran and Lafuente-Monasterio, Maria J. and Lee, Anna and Meister, Stephan and Nislow, Corey and Overington, John P. and Papadatos, George and Patiny, Luc and Pham, James and Ralph, Stuart A. and Ruecker, Andrea and Ryan, Eileen and Southan, Christopher and Srivastava, Kumkum and Swain, Chris and Tarnowski, Matthew J. and Thomson, Patrick and Turner, Peter and Wallace, Iain M. and Wells, Timothy N. C. and White, Karen and White, Laura and Willis, Paul and Winzeler, Elizabeth A. and Wittlin, Sergio and Todd, Matthew H.. (2016) Open source drug discovery : highly potent antimalarial compounds derived from the tres cantos arylpyrroles. ACS central science, 2 (10). pp. 687-701.

Norcross, Neil R. and Baragaña, Beatriz and Wilson, Caroline and Hallyburton, Irene and Osuna-Cabello, Maria and Norval, Suzanne and Riley, Jennifer and Stojanovski, Laste and Simeons, Frederick R. C. and Porzelle, Achim and Grimaldi, Raffaella and Wittlin, Sergio and Duffy, Sandra and Avery, Vicky M. and Meister, Stephan and Sanz, Laura and Jiménez-Díaz, Belén and Angulo-Barturen, Iñigo and Ferrer, Santiago and Martínez, María Santos and Gamo, Francisco Javier and Frearson, Julie A. and Gray, David W. and Fairlamb, Alan H. and Winzeler, Elizabeth A. and Waterson, David and Campbell, Simon F. and Willis, Paul and Read, Kevin D. and Gilbert, Ian H.. (2016) Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials. Journal of Medicinal Chemistry, 59 (13). pp. 6101-6120.

2015

Phillips, Margaret A. and Lotharius, Julie and Marsh, Kennan and White, John and Dayan, Anthony and White, Karen L. and Njoroge, Jacqueline W. and El Mazouni, Farah and Lao, Yanbin and Kokkonda, Sreekanth and Tomchick, Diana R. and Deng, Xiaoyi and Laird, Trevor and Bhatia, Sangeeta N. and March, Sandra and Ng, Caroline L. and Fidock, David A. and Wittlin, Sergio and Lafuente-Monasterio, Maria and Benito, Francisco Javier Gamo and Alonso, Laura Maria Sanz and Martinez, Maria Santos and Jimenez-Diaz, Maria Belen and Bazaga, Santiago Ferrer and Angulo-Barturen, Iñigo and Haselden, John N. and Louttit, James and Cui, Yi and Sridhar, Arun and Zeeman, Anna-Marie and Kocken, Clemens and Sauerwein, Robert and Dechering, Koen and Avery, Vicky M. and Duffy, Sandra and Delves, Michael and Sinden, Robert and Ruecker, Andrea and Wickham, Kristina S. and Rochford, Rosemary and Gahagen, Janet and Iyer, Lalitha and Riccio, Ed and Mirsalis, Jon and Bathhurst, Ian and Rueckle, Thomas and Ding, Xavier and Campo, Brice and Leroy, Didier and Rogers, M. John and Rathod, Pradipsinh K. and Burrows, Jeremy N. and Charman, Susan A.. (2015) A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Science translational medicine, Vol. 7, H. 296 , 296ra111.

Baragaña, Beatriz and Hallyburton, Irene and Lee, Marcus C. S. and Norcross, Neil R. and Grimaldi, Raffaella and Otto, Thomas D. and Proto, William R. and Blagborough, Andrew M. and Meister, Stephan and Wirjanata, Grennady and Ruecker, Andrea and Upton, Leanna M. and Abraham, Tara S. and Almeida, Mariana J. and Pradhan, Anupam and Porzelle, Achim and Martínez, María Santos and Bolscher, Judith M. and Woodland, Andrew and Norval, Suzanne and Zuccotto, Fabio and Thomas, John and Simeons, Frederick and Stojanovski, Laste and Osuna-Cabello, Maria and Brock, Paddy M. and Churcher, Tom S. and Sala, Katarzyna A. and Zakutansky, Sara E. and Jiménez-Díaz, María Belén and Sanz, Laura Maria and Riley, Jennifer and Basak, Rajshekhar and Campbell, Michael and Avery, Vicky M. and Sauerwein, Robert W. and Dechering, Koen J. and Noviyanti, Rintis and Campo, Brice and Frearson, Julie A. and Angulo-Barturen, Iñigo and Ferrer-Bazaga, Santiago and Gamo, Francisco Javier and Wyatt, Paul G. and Leroy, Didier and Siegl, Peter and Delves, Michael J. and Kyle, Dennis E. and Wittlin, Sergio and Marfurt, Jutta and Price, Ric N. and Sinden, Robert E. and Winzeler, Elizabeth A. and Charman, Susan A. and Bebrevska, Lidiya and Gray, David W. and Campbell, Simon and Fairlamb, Alan H. and Willis, Paul A. and Rayner, Julian C. and Fidock, David A. and Read, Kevin D. and Gilbert, Ian H.. (2015) A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature, Vol. 522, H. 7556. pp. 315-320.

Le Manach, Claire and Paquet, Tanya and Brunschwig, Christel and Njoroge, Mathew and Han, Ze and Gonzàlez Cabrera, Diego and Bashyam, Sridevi and Dhinakaran, Rajkumar and Taylor, Dale and Reader, Janette and Botha, Mariette and Churchyard, Alisje and Lauterbach, Sonja and Coetzer, Theresa L. and Birkholtz, Lyn-Marie and Meister, Stephan and Winzeler, Elizabeth A. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Jiménez-Díaz, María-Belén and Santos Martínez, María and Ferrer, Santiago and Angulo-Barturen, Iñigo and Street, Leslie J. and Chibale, Kelly. (2015) A novel pyrazolopyridine with in vivo activity in Plasmodium berghei- and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines. Journal of medicinal chemistry, 58 (21). pp. 8713-8722.

Ongarora, Dennis S. B. and Strydom, Natasha and Wicht, Kathryn and Njoroge, Mathew and Wiesner, Lubbe and Egan, Timothy J. and Wittlin, Sergio and Jurva, Ulrik and Masimirembwa, Collen M. and Chibale, Kelly. (2015) Antimalarial benzoheterocyclic 4-aminoquinolines : structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. Bioorganic & medicinal chemistry, 23 (17). pp. 5419-5432.

Jortzik, Esther and Zocher, Kathleen and Isernhagen, Antje and Mailu, Boniface M. and Rahlfs, Stefan and Viola, Giampietro and Wittlin, Sergio and Hunt, Nicholas H. and Ihmels, Heiko and Becker, Katja. (2015) Benzo[b]quinolizinium derivatives have a strong antimalarial activity and inhibit indoleamine dioxygenase. Antimicrobial agents and chemotherapy, 60 (1). pp. 115-125.

Malmquist, Nicholas A. and Sundriyal, Sandeep and Caron, Joachim and Chen, Patty and Witkowski, Benoit and Menard, Didier and Suwanarusk, Rossarin and Renia, Laurent and Nosten, Francois and Jiménez-Díaz, María Belén and Angulo-Barturen, Iñigo and Martínez, María Santos and Ferrer, Santiago and Sanz, Laura M. and Gamo, Francisco-Javier and Wittlin, Sergio and Duffy, Sandra and Avery, Vicky M. and Ruecker, Andrea and Delves, Michael J. and Sinden, Robert E. and Fuchter, Matthew J. and Scherf, Artur. (2015) Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans. Antimicrobial agents and chemotherapy, Vol. 59, H. 2. pp. 950-959.

Chugh, Monika and Scheurer, Christian and Sax, Sibylle and Bilsland, Elizabeth and van Schalkwyk, Donelly A. and Wicht, Kathryn J. and Hofmann, Natalie and Sharma, Anil and Bashyam, Sridevi and Singh, Shivendra and Oliver, Stephen G. and Egan, Timothy J. and Malhotra, Pawan and Sutherland, Colin J. and Beck, Hans-Peter and Wittlin, Sergio and Spangenberg, Thomas and Ding, Xavier C.. (2015) Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains. Antimicrobial agents and chemotherapy, Vol. 59, H. 2. pp. 1110-1118.

Witschel, Matthias C. and Rottmann, Matthias and Schwab, Anatol and Leartsakulpanich, Ubolsree and Chitnumsub, Penchit and Seet, Michael and Tonazzi, Sandro and Schwertz, Geoffrey and Stelzer, Frank and Mietzner, Thomas and McNamara, Case and Thater, Frank and Freymond, Céline and Jaruwat, Aritsara and Pinthong, Chatchadaporn and Riangrungroj, Pinpunya and Oufir, Mouhssin and Hamburger, Matthias and Mäser, Pascal and Sanz-Alonso, Laura M. and Charman, Susan and Wittlin, Sergio and Yuthavong, Yongyuth and Chaiyen, Pimchai and Diederich, François. (2015) Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT) : co-crystal structures of pyrazolopyrans with potent blood-and liver-stage activities. Journal of Medicinal Chemistry, 58 (7). pp. 3117-3130.

Brücher, Karin and Gräwert, Tobias and Konzuch, Sarah and Held, Jana and Lienau, Claudia and Behrendt, Christoph and Illarionov, Boris and Maes, Louis and Bacher, Adelbert and Wittlin, Sergio and Mordmüller, Benjamin and Fischer, Markus and Kurz, Thomas. (2015) Prodrugs of reverse fosmidomycin analogues. Journal of medicinal chemistry, 58 (4). pp. 2025-2035.

Rusman, Yudi and Held, Benjamin W. and Blanchette, Robert A. and Wittlin, Sergio and Salomon, Christine E.. (2015) Soudanones A-G : antifungal isochromanones from the ascomycetous fungus Cadophora sp. isolated from an iron mine. Journal of natural products, Vol. 78, H. 6. pp. 1456-1460.

Gonzàlez Cabrera, Diego and Douelle, Frederic and Le Manach, Claire and Han, Ze and Paquet, Tanya and Taylor, Dale and Njoroge, Mathew and Lawrence, Nina and Wiesner, Lubbe and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Street, Leslie J. and Chibale, Kelly. (2015) Structure-activity relationship studies of orally active antimalarial 2,4-diamino-thienopyrimidines. Journal of medicinal chemistry, 58 (18). pp. 7572-7579.

2014

González Cabrera, Diego and Le Manach, Claire and Douelle, Frederic and Younis, Yassir and Feng, Tzu-Shean and Paquet, Tanya and Nchinda, Aloysius T. and Street, Leslie J. and Taylor, Dale and de Kock, Carmen and Wiesner, Lubbe and Duffy, Sandra and White, Karen L. and Zabiulla, K. Mohammed and Sambandan, Yuvaraj and Bashyam, Sridevi and Waterson, David and Witty, Michael J. and Charman, Susan A. and Avery, Vicky M. and Wittlin, Sergio and Chibale, Kelly. (2014) 2,4-diaminothienopyrimidines as orally active antimalarial agents. Journal of medicinal chemistry, 57 (3). pp. 1014-1022.

Leven, Michael and Held, Jana and Duffy, Sandra and Tschan, Serena and Sax, Sibylle and Kamber, Jolanda and Frank, Walter and Kuna, Krystina and Geffken, Detlef and Siethoff, Christoph and Barth, Stéphane and Avery, Vicky M. and Wittlin, Sergio and Mordmüller, Benjamin and Kurz, Thomas. (2014) Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides. Journal of medicinal chemistry, 57 (19). pp. 7971-7976.

Le Manach, Claire and Gonzàlez Cabrera, Diego and Douelle, Frederic and Nchinda, Aloysius T. and Younis, Yassir and Taylor, Dale and Wiesner, Lubbe and White, Karen L. and Ryan, Eileen and March, Corinne and Duffy, Sandra and Avery, Vicky M. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Charman, Susan A. and Street, Leslie J. and Chibale, Kelly. (2014) Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library : part 1. Journal of medicinal chemistry, 57 (6). pp. 2789-2798.

Le Manach, Claire and Paquet, Tanya and Gonzàlez Cabrera, Diego and Younis, Yassir and Taylor, Dale and Wiesner, Lubbe and Lawrence, Nina and Schwager, Sylva and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Street, Leslie J. and Chibale, Kelly. (2014) Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library : part 2. Journal of medicinal chemistry, 57 (21). pp. 8839-8848.

Mizukawa, Yuki and Ge, Jian-Feng and Bakar Md, Abu and Itoh, Isamu and Scheurer, Christian and Wittlin, Sergio and Brun, Reto and Matsuoka, Hiroyuki and Ihara, Masataka. (2014) Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites. Bioorganic & medicinal chemistry, 22 (14). pp. 3749-3752.

2013

Le Manach, Claire and Scheurer, Christian and Sax, Sibylle and Schleiferböck, Sarah and Gonzalez Cabrera, Diego and Younis, Yassir and Paquet, Tanya and Street, Leslie and Smith, Peter and Ding, Xavier and Waterson, David and Witty, Michael J. and Leroy, Didier and Chibale, Kelly and Wittlin, Sergio. (2013) Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum. Malaria journal, Vol. 12 , 424.

Schleiferböck, Sarah and Scheurer, Christian and Ihara, Masataka and Itoh, Isamu and Bathurst, Ian and Burrows, Jeremy N. and Fantauzzi, Pascal and Lotharius, Julie and Charman, Susan A. and Morizzi, Julia and Shackleford, David M. and White, Karen L. and Brun, Reto and Wittlin, Sergio. (2013) In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models. Drug design, development and therapy, Vol. 7. pp. 1377-1384.

Abiodun, Oyindamola O. and Brun, Reto and Wittlin, Sergio. (2013) In vitro interaction of artemisinin derivatives or the fully synthetic peroxidic anti-malarial OZ277 with thapsigargin in Plasmodium falciparum strains. Malaria journal, Vol. 12 , 43.

Hao, Hong-Dong and Wittlin, Sergio and Wu, Yikang. (2013) Potent antimalarial 1,2,4-trioxanes through perhydrolysis of epoxides. Chemistry : a European journal, Vol. 19, H. 23. pp. 7605-7619.

Nsumiwa, Samkele and Kuter, David and Wittlin, Sergio and Chibale, Kelly and Egan, Timothy J.. (2013) Structure-activity relationships for ferriprotoporphyrin IX association and β-hematin inhibition by 4-aminoquinolines using experimental and ab initio methods. Bioorganic & medicinal chemistry, 21 (13). pp. 3738-3748.

Younis, Yassir and Douelle, Frederic and González Cabrera, Diego and Le Manach, Claire and Nchinda, Aloysius T. and Paquet, Tanya and Street, Leslie J. and White, Karen L. and Zabiulla, K. Mohammed and Joseph, Jayan T. and Bashyam, Sridevi and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Charman, Susan A. and Chibale, Kelly. (2013) Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity. Journal of medicinal chemistry, 56 (21). pp. 8860-8871.

2011

Baschong, Werner and Wittlin, Sergio and Inglis, Kirstine A. and Fairlamb, Alan H. and Croft, Simon L. and Kumar, T. R. Santha and Fidock, David A. and Brun, Reto. (2011) Triclosan is minimally effective in rodent malaria models. Nature medicine, Vol. 17. pp. 33-34.

2009

Nyongbela, Kennedy and Ndjoko, Karine Ioset and Brun, Reto and Wittlin, Sergio and Mbah, James and Makolo, Felix and Akam, Marc and Wirmum, Claire and Efange, Simon and Hostettmann, Kurt. (2009) Occurrence of sesquiterpene derivatives in Scleria striatonux de wild (Cyperaceae). Natural product communications : NPC, Vol. 4, H. 1. pp. 5-8.

This list was generated on Mon Sep 26 23:34:37 2022 CEST.