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Refereed Journals

2020

   
[261] Current advances in the clinical development of anti-tubercular agents S. R. Tetali, E. Kunapaeddi, R. P. Mailavaram, V. Singh, P. Borah, P. K. Deb, K. N. Venugopala, W. Hourani, R. K. Tekade.  Tuberculois 2020 125, 101989
[260] Potentiation of rifampin activity in a mouse model of tuberculosis by activation of host transcription factor EB.  R. Bryk*, S. Mundhra, X. Jiang, M. Wood, D. Pfau, E. Weber, S. Park, L. Zhang, C. Wilson, L. Street, K. Chibale, M. Zimmerman, V. Dartois, N. Pastore, A. Ballabio, N. Hawryluk, S. Canan, J. Zeldis, V. Khetani, J.Camardo, and C. Nathan PLoS Pathog 2020, 16(6): e1008567
[259] Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity. M. Vanaerschot, J. M. Murithi, C. Flerida, A. Pasaje, S. Ghidelli-Disse, L. Dwomoh, M. Bird, N. Spottiswoode, N. Mittal, L. B. Arendse, E. S. Owen, K. J. Wicht, G. Siciliano, M. Bo¨ sche, T. Yeo, T.R. Santha Kumar, S. Mok, E. F. Carpenter, M. J. Giddins, O. Sanz, S. Ottilie, P. Alano, K. Chibale, M. Llina´ s, A-C Uhlemann, M. Delves, A. B. Tobin, C Doerig, E. A. Winzeler, M. C. S. Lee, J. C. Niles and D. A. Fidock.  Cell Chem Biol 2020   27, 806–816
[258] A diverse view of science to catalyse change.  C. A. Urbina-Blanco, S. Z. Jilani, I. R. Speight, M. J. Bojdys, T. Friščić, J. Fraser Stoddart, T. L. Nelson, J. Mack, R. A. S. Robinson, E. A. Waddell, J. L. Lutkenhaus, M. Godfrey, M. I. Abboud, S. O. Aderinto, D. Aderohunmu, L. Bibič, J. Borges, V. M. Dong, L. Ferrins, F. Man Fung, T. John, F. P. L. Lim, S. L. Masters, D. Mambwe, P. Thordarson, M-M. Titirici, G. D. Tormet-González, M. M. Unterlass, A. Wadle, V. W.-W. Yam and Y-W. Yang. Nature Chemistry 2020 12, 773–776
[257] Antimicrobial evaluation of neutral and cationic iridium(III) and rhodium(III) aminoquinoline-benzimidazole hybrid complexes*. N. Baartzes, A. Jordaan, D. F. Warner, J. Combrinck, D. Taylor, K. Chibale and G. S. Smith.  Eur J Med Chem 2020 206, 112694
[256] Synthesis, Structure−Activity Relationship, and Mechanistic Studies of Aminoquinazolinones Displaying Antimycobacterial Activity.  J.N. Akester, P. Njaria, A. Nchinda, C. Le Manach, A. Myrick, V. Singh, N. Lawrence, M. Njoroge, D. Taylor, A. Moosa, A. J. Smith, E. J. Brooks, A. J. Lenaerts, G. T. Robertson, T. R. Ioerger, R. Mueller and K. Chibale.  ACS Infect Dis 2020, 6, 7, 1951–1964
[255] Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity. K. Singh, G. Kaur, P. S. Shanika, G. A Dziwornu, J. Okombo, K. Chibale.  Biorg & Med Chem 2020 28 115530
[254] Design, synthesis and characterization of novel 2-(2, 3-dichlorophenyl)-5-aryl-1,3,4-oxadiazole derivatives for their anti-tubercular activity against Mycobacterium tuberculosis.  R. Ningegowda, S. Chandrashekharappa, V. Singh, V. Mohanlall and K. N. Venugopala.  Chem Data Collections 2020 28 100431
[253] Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?  G.A. Dziwornu, H.D. Attram, S. Gachuhi and K. Chibale. RSC Med Chem2020  11, 455  
[252] Synthesis and evaluation of the performance of a small molecule library based on diverse tropane-related scaffolds.  R.A. Lowe, D. Taylor, K. Chibale, A. Nelson* and S.P. Marsden.  Biorg Med Chem 2020.  28, 115442 
[251] Synthesis and biological evaluation of novel quinoline-piperidine scaffolds as antiplasmodium agents.  T. Van deWalle; M. Boone; J. Van Puyvelde; J. Combrinck; P.J. Smith; K. Chibale; S. Mangelinck and M. D’hooghe.  Eur J Med Chem. 2020.  198, 112330
[250] Pharmacokinetics and Organ Distribution of C-3 Alkyl Esters as Potential Antimycobacterial Prodrugs of Fusidic Acid N Strydom, G Kaur, GA Dziwornu, J Okombo, L Wiesner, K Chibale.  ACS Infectious Diseases 2020, 6, 459-466
[249] Quest for the holy Grail.  Huszar, Singh and Chibale Drug Discovery Today  2020
[248] Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present). P. M. Cheuka, G. Dziwornu, J. Okombo, and K. Chibale* J. Med. Chem. 2020
[247] Safety, tolerability, pharmacokinetics and antimalarial activity of the novel Plasmodium phosphatidylinositol 4-kinase inhibitor MMV390048 in healthy volunteers.  P. Sinxadi, C. Donini, H. Johnstone, G. Langdon, L. Wiesner, E. Allen, S. Duparc, S. Chalon, J. McCarthy, U. Lorch, K. Chibale, J. Möhrle, and K. Barnes*. Antimicrob. Agents Chemother. 2020
[246] Combining stage specificity and metabolomic profiling to advance antimalarial drug discovery. J. M. Murithi, E. S. Owen, E. S. Istvan, M. C.S. Lee, S. Otillie, K. Chibale, D. E. Goldberg, E. A. Winzeler, M. Llinás, D.A. Fidock*, M. Vanaerschot* Cell Chemical Biology. 2020,
[245] A preformulation co-crystal screening case study: polymorphic co-crystals of an imidazopyridazine antimalarial drug lead with the coformer succinic acid.  T.J. Noonan, K. Chibale, S. A. Bourne, M. R. Caira* Journal of Molecular Structure 2020, 1204-127561