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Page 1
2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy.
Dziwornu GA, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu VS, Samanta S, Bhana AD, Korkor CM, Garnie LF, Teixeira N, Wicht KJ, Taylor D, Olckers R, Njoroge M, Gibhard L, Salomane N, Wittlin S, Mahato R, Chakraborty A, Sevilleno N, Coyle R, Lee MCS, Godoy LC, Pasaje CF, Niles JC, Reader J, van der Watt M, Birkholtz LM, Bolscher JM, de Bruijni MHC, Coulson LB, Basarab GS, Ghorpade SR, Chibale K. Dziwornu GA, et al. Among authors: ghorpade sr. J Med Chem. 2024 Jul 11;67(13):11401-11420. doi: 10.1021/acs.jmedchem.4c01154. Epub 2024 Jun 25. J Med Chem. 2024. PMID: 38918002 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: ghorpade sr. 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.
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: ghorpade sr. 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.
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
Govender P, Müller R, Singh K, Reddy V, Eyermann CJ, Fienberg S, Ghorpade SR, Koekemoer L, Myrick A, Schnappinger D, Engelhart C, Meshanni J, Byl JAW, Osheroff N, Singh V, Chibale K, Basarab GS. Govender P, et al. Among authors: ghorpade sr. J Med Chem. 2022 May 12;65(9):6903-6925. doi: 10.1021/acs.jmedchem.2c00266. Epub 2022 May 2. J Med Chem. 2022. PMID: 35500229 Free PMC article.
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: ghorpade sr. 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.
Spiropyrimidinetriones: a Class of DNA Gyrase Inhibitors with Activity against Mycobacterium tuberculosis and without Cross-Resistance to Fluoroquinolones.
Basarab GS, Ghorpade S, Gibhard L, Mueller R, Njoroge M, Peton N, Govender P, Massoudi LM, Robertson GT, Lenaerts AJ, Boshoff HI, Joerss D, Parish T, Durand-Reville TF, Perros M, Singh V, Chibale K. Basarab GS, et al. Antimicrob Agents Chemother. 2022 Apr 19;66(4):e0219221. doi: 10.1128/aac.02192-21. Epub 2022 Mar 10. Antimicrob Agents Chemother. 2022. PMID: 35266826 Free PMC article.
1,3-Diarylpyrazolyl-acylsulfonamides Target HadAB/BC Complex in Mycobacterium tuberculosis.
Singh V, Grzegorzewicz AE, Fienberg S, Müller R, Khonde LP, Sanz O, Alfonso S, Urones B, Drewes G, Bantscheff M, Ghidelli-Disse S, Ioerger TR, Angala B, Liu J, Lee RE, Sacchettini JC, Krieger IV, Jackson M, Chibale K, Ghorpade SR. Singh V, et al. Among authors: ghorpade sr. ACS Infect Dis. 2022 Nov 11;8(11):2315-2326. doi: 10.1021/acsinfecdis.2c00392. Epub 2022 Nov 3. ACS Infect Dis. 2022. PMID: 36325756 Free PMC article.
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR. Naik M, et al. Among authors: ghorpade sr. J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24871036
Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B.
Kale MG, Raichurkar A, P SH, Waterson D, McKinney D, Manjunatha MR, Kranthi U, Koushik K, Jena Lk, Shinde V, Rudrapatna S, Barde S, Humnabadkar V, Madhavapeddi P, Basavarajappa H, Ghosh A, Ramya VK, Guptha S, Sharma S, Vachaspati P, Kumar KN, Giridhar J, Reddy J, Panduga V, Ganguly S, Ahuja V, Gaonkar S, Kumar CN, Ogg D, Tucker JA, Boriack-Sjodin PA, de Sousa SM, Sambandamurthy VK, Ghorpade SR. Kale MG, et al. Among authors: ghorpade sr. J Med Chem. 2013 Nov 14;56(21):8834-48. doi: 10.1021/jm401268f. Epub 2013 Oct 18. J Med Chem. 2013. PMID: 24088190
17 results