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The Tuberculosis Drug Accelerator at year 10: what have we learned?
Aldridge BB, Barros-Aguirre D, Barry CE 3rd, Bates RH, Berthel SJ, Boshoff HI, Chibale K, Chu XJ, Cooper CB, Dartois V, Duncan K, Fotouhi N, Gusovsky F, Hipskind PA, Kempf DJ, Lelièvre J, Lenaerts AJ, McNamara CW, Mizrahi V, Nathan C, Olsen DB, Parish T, Petrassi HM, Pym A, Rhee KY, Robertson GT, Rock JM, Rubin EJ, Russell B, Russell DG, Sacchettini JC, Schnappinger D, Schrimpf M, Upton AM, Warner P, Wyatt PG, Yuan Y. Aldridge BB, et al. Among authors: chibale k. Nat Med. 2021 Aug;27(8):1333-1337. doi: 10.1038/s41591-021-01442-2. Nat Med. 2021. PMID: 34226736 Free PMC article.
Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization.
Soares de Melo C, Feng TS, van der Westhuyzen R, Gessner RK, Street LJ, Morgans GL, Warner DF, Moosa A, Naran K, Lawrence N, Boshoff HI, Barry CE 3rd, Harris CJ, Gordon R, Chibale K. Soares de Melo C, et al. Among authors: chibale k. Bioorg Med Chem. 2015 Nov 15;23(22):7240-50. doi: 10.1016/j.bmc.2015.10.021. Epub 2015 Oct 22. Bioorg Med Chem. 2015. PMID: 26522089
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda A, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden P, Harris CJ, Gordon R, Ghidelli-Disse S, Pflaumer H, Boesche M, Drewes G, Sanz O, Santos G, Rebollo-Lopez MJ, Urones B, Selenski C, Lafuente-Monasterio MJ, Axtman M, Lelièvre J, Ballell L, Mueller R, Street LJ, Ghorpade SR, Chibale K. Wilson CR, et al. Among authors: chibale k. J Med Chem. 2017 Dec 28;60(24):10118-10134. doi: 10.1021/acs.jmedchem.7b01347. Epub 2017 Dec 7. J Med Chem. 2017. PMID: 29148755 Free PMC article.
2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization.
Murugesan D, Ray PC, Bayliss T, Prosser GA, Harrison JR, Green K, Soares de Melo C, Feng TS, Street LJ, Chibale K, Warner DF, Mizrahi V, Epemolu O, Scullion P, Ellis L, Riley J, Shishikura Y, Ferguson L, Osuna-Cabello M, Read KD, Green SR, Lamprecht DA, Finin PM, Steyn AJC, Ioerger TR, Sacchettini J, Rhee KY, Arora K, Barry CE 3rd, Wyatt PG, Boshoff HIM. Murugesan D, et al. Among authors: chibale k. ACS Infect Dis. 2018 Jun 8;4(6):954-969. doi: 10.1021/acsinfecdis.7b00275. Epub 2018 Mar 26. ACS Infect Dis. 2018. PMID: 29522317 Free PMC article.
Synthesis, Structure-Activity Relationship, and Mechanistic Studies of Aminoquinazolinones Displaying Antimycobacterial Activity.
Akester JN, Njaria P, Nchinda A, Le Manach C, Myrick A, Singh V, Lawrence N, Njoroge M, Taylor D, Moosa A, Smith AJ, Brooks EJ, Lenaerts AJ, Robertson GT, Ioerger TR, Mueller R, Chibale K. Akester JN, et al. Among authors: chibale k. ACS Infect Dis. 2020 Jul 10;6(7):1951-1964. doi: 10.1021/acsinfecdis.0c00252. Epub 2020 Jun 15. ACS Infect Dis. 2020. PMID: 32470286 Free PMC article.
Potentiation of rifampin activity in a mouse model of tuberculosis by activation of host transcription factor EB.
Bryk R, Mundhra S, Jiang X, Wood M, Pfau D, Weber E, Park S, Zhang L, Wilson C, Van der Westhuyzen R, Street L, Chibale K, Zimmerman M, Dartois V, Pastore N, Ballabio A, Hawryluk N, Canan S, Khetani V, Camardo J, Nathan C. Bryk R, et al. Among authors: chibale k. PLoS Pathog. 2020 Jun 23;16(6):e1008567. doi: 10.1371/journal.ppat.1008567. eCollection 2020 Jun. PLoS Pathog. 2020. PMID: 32574211 Free PMC article.
Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.
Soares de Melo C, Singh V, Myrick A, Simelane SB, Taylor D, Brunschwig C, Lawrence N, Schnappinger D, Engelhart CA, Kumar A, Parish T, Su Q, Myers TG, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden PD, Buchanan KI, Bayliss T, Green SR, Ray PC, Wyatt PG, Basarab GS, Eyermann CJ, Chibale K, Ghorpade SR. Soares de Melo C, et al. Among authors: chibale k. J Med Chem. 2021 Jan 14;64(1):719-740. doi: 10.1021/acs.jmedchem.0c01727. Epub 2021 Jan 4. J Med Chem. 2021. PMID: 33395287 Free PMC article.
MalDA, Accelerating Malaria Drug Discovery.
Yang T, Ottilie S, Istvan ES, Godinez-Macias KP, Lukens AK, Baragaña B, Campo B, Walpole C, Niles JC, Chibale K, Dechering KJ, Llinás M, Lee MCS, Kato N, Wyllie S, McNamara CW, Gamo FJ, Burrows J, Fidock DA, Goldberg DE, Gilbert IH, Wirth DF, Winzeler EA; Malaria Drug Accelerator Consortium. Yang T, et al. Among authors: chibale k. Trends Parasitol. 2021 Jun;37(6):493-507. doi: 10.1016/j.pt.2021.01.009. Epub 2021 Feb 26. Trends Parasitol. 2021. PMID: 33648890 Free PMC article. Review.
279 results