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Page 1
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: nchinda a. 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.
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: nchinda a. 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.
Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines.
González Cabrera D, Douelle F, Younis Y, Feng TS, Le Manach C, Nchinda AT, Street LJ, Scheurer C, Kamber J, White KL, Montagnat OD, Ryan E, Katneni K, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Charman SA, Wittlin S, Chibale K. González Cabrera D, et al. Among authors: nchinda at. J Med Chem. 2012 Dec 27;55(24):11022-30. doi: 10.1021/jm301476b. Epub 2012 Dec 14. J Med Chem. 2012. PMID: 23189922
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.
Younis Y, Douelle F, González Cabrera D, Le Manach C, Nchinda AT, Paquet T, Street LJ, White KL, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K. Younis Y, et al. Among authors: nchinda at. J Med Chem. 2013 Nov 14;56(21):8860-71. doi: 10.1021/jm401278d. Epub 2013 Oct 29. J Med Chem. 2013. PMID: 24099149
2,4-Diaminothienopyrimidines as orally active antimalarial agents.
González Cabrera D, Le Manach C, Douelle F, Younis Y, Feng TS, Paquet T, Nchinda AT, Street LJ, Taylor D, de Kock C, Wiesner L, Duffy S, White KL, Zabiulla KM, Sambandan Y, Bashyam S, Waterson D, Witty MJ, Charman SA, Avery VM, Wittlin S, Chibale K. González Cabrera D, et al. Among authors: nchinda at. J Med Chem. 2014 Feb 13;57(3):1014-22. doi: 10.1021/jm401760c. Epub 2014 Jan 28. J Med Chem. 2014. PMID: 24446664
Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.
Le Manach C, Gonzàlez Cabrera D, Douelle F, Nchinda AT, Younis Y, Taylor D, Wiesner L, White KL, Ryan E, March C, Duffy S, Avery VM, Waterson D, Witty MJ, Wittlin S, Charman SA, Street LJ, Chibale K. Le Manach C, et al. Among authors: nchinda at. J Med Chem. 2014 Mar 27;57(6):2789-98. doi: 10.1021/jm500098s. Epub 2014 Mar 13. J Med Chem. 2014. PMID: 24568587
Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.
Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K. Nchinda AT, et al. J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27. J Med Chem. 2018. PMID: 29665687
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.
Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K. Le Manach C, et al. Among authors: nchinda at. J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16. J Med Chem. 2018. PMID: 30256636
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.
Horatscheck A, Andrijevic A, Nchinda AT, Le Manach C, Paquet T, Khonde LP, Dam J, Pawar K, Taylor D, Lawrence N, Brunschwig C, Gibhard L, Njoroge M, Reader J, van der Watt M, Wicht K, de Sousa ACC, Okombo J, Maepa K, Egan TJ, Birkholtz LM, Basarab GS, Wittlin S, Fish PV, Street LJ, Duffy J, Chibale K. Horatscheck A, et al. Among authors: nchinda at. J Med Chem. 2020 Nov 12;63(21):13013-13030. doi: 10.1021/acs.jmedchem.0c01411. Epub 2020 Oct 25. J Med Chem. 2020. PMID: 33103428 Free PMC article.
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis.
Khonde LP, Müller R, Boyle GA, Reddy V, Nchinda AT, Eyermann CJ, Fienberg S, Singh V, Myrick A, Abay E, Njoroge M, Lawrence N, Su Q, Myers TG, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden PD, Massoudi LM, Robertson GT, Lenaerts AJ, Basarab GS, Ghorpade SR, Chibale K. Khonde LP, et al. Among authors: nchinda at. J Med Chem. 2021 Sep 9;64(17):12790-12807. doi: 10.1021/acs.jmedchem.1c00837. Epub 2021 Aug 20. J Med Chem. 2021. PMID: 34414766 Free PMC article.
27 results