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Page 1
Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth.
Ray PC, Huggett M, Turner PA, Taylor M, Cleghorn LAT, Early J, Kumar A, Bonnett SA, Flint L, Joerss D, Johnson J, Korkegian A, Mullen S, Moure AL, Davis SH, Murugesan D, Mathieson M, Caldwell N, Engelhart CA, Schnappinger D, Epemolu O, Zuccotto F, Riley J, Scullion P, Stojanovski L, Massoudi L, Robertson GT, Lenaerts AJ, Freiberg G, Kempf DJ, Masquelin T, Hipskind PA, Odingo J, Read KD, Green SR, Wyatt PG, Parish T. Ray PC, et al. ACS Omega. 2021 Jan 13;6(3):2284-2311. doi: 10.1021/acsomega.0c05589. eCollection 2021 Jan 26. ACS Omega. 2021. PMID: 33521468 Free PMC article.
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI. Park Y, et al. Among authors: ray pc. ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17. ACS Infect Dis. 2017. PMID: 27704782 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: ray pc. 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.
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
Cleghorn LAT, Ray PC, Odingo J, Kumar A, Wescott H, Korkegian A, Masquelin T, Lopez Moure A, Wilson C, Davis S, Huggett M, Turner P, Smith A, Epemolu O, Zuccotto F, Riley J, Scullion P, Shishikura Y, Ferguson L, Rullas J, Guijarro L, Read KD, Green SR, Hipskind P, Parish T, Wyatt PG. Cleghorn LAT, et al. Among authors: ray pc. J Med Chem. 2018 Aug 9;61(15):6592-6608. doi: 10.1021/acs.jmedchem.8b00172. Epub 2018 Jul 26. J Med Chem. 2018. PMID: 29944372 Free PMC article.
Targeting Mycobacterium tuberculosis CoaBC through Chemical Inhibition of 4'-Phosphopantothenoyl-l-cysteine Synthetase (CoaB) Activity.
Evans JC, Murugesan D, Post JM, Mendes V, Wang Z, Nahiyaan N, Lynch SL, Thompson S, Green SR, Ray PC, Hess J, Spry C, Coyne AG, Abell C, Boshoff HIM, Wyatt PG, Rhee KY, Blundell TL, Barry CE 3rd, Mizrahi V. Evans JC, et al. Among authors: ray pc. ACS Infect Dis. 2021 Jun 11;7(6):1666-1679. doi: 10.1021/acsinfecdis.0c00904. Epub 2021 May 3. ACS Infect Dis. 2021. PMID: 33939919 Free PMC article.
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.
Wilson C, Ray P, Zuccotto F, Hernandez J, Aggarwal A, Mackenzie C, Caldwell N, Taylor M, Huggett M, Mathieson M, Murugesan D, Smith A, Davis S, Cocco M, Parai MK, Acharya A, Tamaki F, Scullion P, Epemolu O, Riley J, Stojanovski L, Lopez-Román EM, Torres-Gómez PA, Toledo AM, Guijarro-Lopez L, Camino I, Engelhart CA, Schnappinger D, Massoudi LM, Lenaerts A, Robertson GT, Walpole C, Matthews D, Floyd D, Sacchettini JC, Read KD, Encinas L, Bates RH, Green SR, Wyatt PG. Wilson C, et al. J Med Chem. 2022 Jan 13;65(1):409-423. doi: 10.1021/acs.jmedchem.1c01586. Epub 2021 Dec 15. J Med Chem. 2022. PMID: 34910486 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: ray pc. 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.
Resistance of Mycobacterium tuberculosis to indole 4-carboxamides occurs through alterations in drug metabolism and tryptophan biosynthesis.
Libardo MDJ, Duncombe CJ, Green SR, Wyatt PG, Thompson S, Ray PC, Ioerger TR, Oh S, Goodwin MB, Boshoff HIM, Barry CE 3rd. Libardo MDJ, et al. Among authors: ray pc. Cell Chem Biol. 2021 Aug 19;28(8):1180-1191.e20. doi: 10.1016/j.chembiol.2021.02.023. Epub 2021 Mar 24. Cell Chem Biol. 2021. PMID: 33765439 Free PMC article.
Prediction of Drug Penetration in Tuberculosis Lesions.
Sarathy JP, Zuccotto F, Hsinpin H, Sandberg L, Via LE, Marriner GA, Masquelin T, Wyatt P, Ray P, Dartois V. Sarathy JP, et al. ACS Infect Dis. 2016 Aug 12;2(8):552-63. doi: 10.1021/acsinfecdis.6b00051. Epub 2016 Jul 6. ACS Infect Dis. 2016. PMID: 27626295 Free PMC article.
171 results