Items where Author is "Chibale, K."

2022

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.

2021

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.

Probst, A. and Chisanga, K. and Dziwornu, G. A. and Häberli, C. and Keiser, J. and Chibale, K.. (2021) Expanding the activity profile of pyrido[1,2-a]benzimidazoles: synthesis and evaluation of novel n(1)-1-phenylethanamine derivatives against Schistosoma mansoni. ACS Infect Dis, 7 (5). pp. 1032-1043.

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.

2020

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

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.

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.

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.

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.

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.

2011

Ndakala, A. J. and Gessner, R. K. and Gitari, P. W. and October, N. and White, K. L. and Hudson, A. and Fakorede, F. and Shackleford, D. M. and Kaiser, M. and Yeates, C. and Charman, S. A. and Chibale, K.. (2011) Antimalarial Pyrido[1,2-a]benzimidazoles. Journal of medicinal chemistry, 54 (13). pp. 4581-4589.

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.