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Refereed Journals

2018

[227] Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.  L. Gibhard, M. Njoroge, T. Paquet, C. Brunschwig, D. Taylor, N. Lawrence, E. Abay, S. Wittlin, L. Wiesner, L. J. Street, K. Chibale, and G. S. Basarab*. Antimicrob. Agents Chemother. 2018, 62 (issue 12), e00261-18
[226] Structure-activity relationship studies of antiplasmodial cyclometallated ruthenium(II), rhodium(III) and iridium(III) complexes of 2-phenylbenzimidazoles.  L. Rylands, A. Welsh, K. Maepa, T. Stringer, D. Taylor, K. Chibale and G. S. Smith∗ Eur. J. Med. Chem, 2019, 161, 11–21
[225] Antimalarial imidazopyridazines: hERG structure-activity relationships and solubility optimization.  P.M. Cheuka, N. Lawrence, D. Taylor, S. Wittlin and K. Chibale*. Med. Chem. Commun., 2018, 9, 1733–1745
[224] The Next Generation Scientist program:capacity-building for future scientific leaders in low- and middle-income countries.  G. Pillai, K. Chibale, E. C. Constable, A. N. Keller*, M. M. Gutierrez, F. Mirza, C. Sengstag, C. Masimirembwa, P. Denti, G. Maartens, M. Ramsay, B. Ogutu, E. Makonnen, R. Gordon, C. Gil Ferreira, F. A. Goldbaum, W.M. S. Degrave, J. Spector, B. Tadmor and H. J. Kaiser. BMC Medical Education, 2018, 18, 233.   https://doi.org/10.1186/s12909-018-1331-y
[223] Plasmodial kinase inhibitors - License to cure?.  D. G.  Cabrera, A. Horatscheck, C. R. Wilson, G. Basarab, C. J. Eyermann and K. Chibale* J. Med. Chem. 2018, 61, 8061−8077
[222] UCT943, a next generation Plasmodium falciparum PI4K inhibitor preclinical candidate for the treatment of malaria.  C. Brunschwig, N. Lawrence, D. Taylor, E. Abay, M. Njoroge, G. S. Basarab, C. Le Manach, T. Paquet, D. G. Cabrera, A. T. Nchinda, C. de Kock, L. Wiesner, P. Denti, D.  Waterson, B. Blasco, D. Leroy, M. J. Witty, C. Donini, J. Duffy, S. Wittlin, K. L. White, S. A. Charman, M. B. Jiménez-Díaz, I. Angulo-Barturen, E. Herreros, F. Javier-Gamo, R. Rochford, D. Mancama, T. L. Coetzer, M. E. van der Watt, J. Reader, L.-M. Birkholtz, K. C. Marsh, S. M. Solapure, J. E. Burke, J.A. McPhail, M. Vanaerschot, D. A. Fidock, P. V. Fish, P. Siegl, D. A. Smith, G. Wirjanata, R.  Noviyanti, R. N. Price, J. Marfurt, K. D. Silue, L. J. Street, and K. Chibale*. Antimicrob. Agents Chemother. 2018, 62 (Issue 9), e00012-18; doi:10.1128/AAC.00012-18
[221] 3D-QSAR Modelling and Synthesis of New Fusidic Acid Derivatives as Antiplasmodial Agents. G.Kaur, E. Pavadai, S. Wittlin and K. Chibale*  J. Chem. Inf. Model. 2018, 58, 1553−1560
[220] Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.  N. Kandepedu, D. G. Cabrera, S. Eedubilli, D. Taylor, C. Brunschwig, L. Gibhard, M. Njoroge, N. Lawrence, T. Paquet, C. J. Eyermann, T. Spangenberg, G. S. Basarab, L. J. Street, and K. Chibale* J. Med. Chem. 2018, 61, 5692 -5703
[219] 2-Mercapto-quinazolinones as inhibitors of NDH-2 and Mycobacterium tuberculosis: Structure-activity relationships, mechanism of action and ADME characterization.  D. Murugesan, P. C. Ray, T. Bayliss, G. A. Prosser, J. R. Harrison, K. Green, C. S. de Melo, T.-S. Feng, L. J. Street, K. Chibale, D. Warner, V. Mizrahi, O. Epemolu, P. Scullion, L. Ellis, J. Riley, Y. Shishikura, L. Ferguson, M. Osuna- Cabello, K. D. Read, S. R. Green, D. A. Lamprecht, P. M. Finin, A.J.C. Steyn, T. R. Ioerger, J. Sacchettini, K. Rhee, K. Arora, C. E. Barry III, P. G. Wyatt,* and H. I.M. Boshoff,*  ACS Infect. Dis. 2018, 4, 954−969 
[218] Identification of fast-acting 2,6-disubstituted imidazopyridines that are efficacious in the in vivo humanized Plasmodium falciparum NODscidIL2Rγnull mouse model of malaria.  A. T. Nchinda, C. Le Manach, T. Paquet, D. G. Cabrera, K. J. Wicht, C. Brunschwig, M. Njoroge, E. Abay, D. Taylor, N. Lawrence, S. Wittlin, M.-B. Jiménez-Díaz, M. S. Martínez, S. Ferrer, I. Angulo-Barturen, M. J. Lafuente-Monasterio, J. Duffy, J. Burrows, L. J. Street and K. Chibale* J. Med. Chem. 2018, 61, 4213−4227.
[217] Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis.  M. A. Martinez-Grau, I. C. G. Valcarcel, J. V. Early, R. K. Gessner, C. S. de Melo, E. M. M. de la Nava, A. Korkegian, Y. Ovechkina, L. Flint, A. Gravelle, J. W. Cramer, P. V. Desai, L. J. Street, J. Odingo, T. Masquelin, K. Chibale, and T. Parish*. Bioorg. Med. Chem. Lett.  2018, 28, 1758–1764
[216] Crystal structures of sampatrilat and sampatrilat-Asp in complex with human ACE: a molecular basis for domain-selectivity G. E. Cozier, S. L. Schwager, R. K. Sharma, K. Chibale, E. D. Sturrock and K. R. Acharya* The FEBS Journal 2018, 285, 1477–1490. JIF = 4.237 Article featured on front cover of the journal issue
[215] Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials.  M. E. van der Watt, J. Reader, A. Churchyard, S. H. Nondaba, S. B. Lauterbach, J. Niemand, S. Abayomi, R.A. van Biljon, J. I. Connacher, R. D. J. van Wyk, C. Le Manach, T. Paquet, D. G. Cabrera, C. Brunschwig, A. Theron, S. Lozano-Arias, J. F. I. Rodrigues, E. Herreros, D. Leroy, J. Duffy, L. J. Street, K. Chibale, D. Mancama, T. L. Coetzer and L.-M. Birkholtz* J Antimicrob Chemother 2018, 73, 1279–1290
[214] Recent updates in the discovery and development of novel antimalarial candidates. J. Okombo and K. Chibale*. MedChemComm, 2018, 9, 590 - 590
[213] Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity.  R. Chopra, K.  Chibale and K. Singh*. Eur. J. Med. Chem, 2018, 148, 39–53.
[212] Reversed Isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis. M. Kumar, K. Singh, A. H. Ngwane, F. Hamzabegovic, G. Abate,, B. Baker, I. Wiid, D. F. Hoft, P. Ruminski, and K. Chibale*  Bioorg. Med. Chem.  2018, 26, 833–844
[211] The Design and Development of a Potent and Selective Novel Diprolyl Derivative that Binds to the N-domain of Angiotensin-I Converting Enzyme.  S. Fienberg, G. Cozier, K. Acharya, K. Chibale*, and E. D. Sturrock*J. Med. Chem. 2018, 61, 344−359