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Page 1
MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity.
Cheng D, Zinker BA, Luo Y, Shipkova P, De Oliveira CH, Krishna G, Brown EA, Boehm SL, Tirucherai GS, Gu H, Ma Z, Chu CH, Onorato JM, Kopcho LM, Ammar R, Smith J, Devasthale P, Lawrence RM, Stryker SA, Dierks EA, Azzara AV, Carayannopoulos L, Charles ED, Lentz KA, Gordon DA. Cheng D, et al. Among authors: devasthale p. Cell Metab. 2022 Nov 1;34(11):1732-1748.e5. doi: 10.1016/j.cmet.2022.10.007. Cell Metab. 2022. PMID: 36323235 Free article.
A simple, inexpensive apparatus for performance of preparative scale solution phase multiple parallel synthesis of drug analogs. II. Biological evaluation of a retrospective library of quinolone antiinfective agents.
Frank KE, Devasthale PV, Gentry EJ, Ravikumar VT, Keschavarz-Shokri A, Mitscher LA, Nilius A, Shen LL, Shawar R, Baker WR. Frank KE, et al. Among authors: devasthale pv. Comb Chem High Throughput Screen. 1998 Jun;1(2):89-99. Comb Chem High Throughput Screen. 1998. PMID: 10500768
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.
Devasthale P, Wang W, Hernandez AS, Moore F, Renduchintala K, Sridhar R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Li YX, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2793-9. doi: 10.1016/j.bmcl.2015.05.008. Epub 2015 May 15. Bioorg Med Chem Lett. 2015. PMID: 26022839
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.
Devasthale P, Wang W, Mignone J, Renduchintala K, Radhakrishnan S, Dhanapal J, Selvaraj J, Kuppusamy R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4412-8. doi: 10.1016/j.bmcl.2015.09.018. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26386604
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY, Mathur A, Hou X, Kempson J, Wu DR, Li YX, Azzara AV, Ma Z, Chu CH, Chen L, Cullen MJ, Rooney S, Harvey S, Kopcho L, Panemangelor R, Abell L, O'Malley K, Keim WJ, Dierks E, Chang S, Foster K, Apedo A, Harden D, Dabros M, Gao Q, Pelleymounter MA, Whaley JM, Robl JA, Cheng D, Lawrence RM, Devasthale P. Turdi H, et al. Among authors: devasthale p. J Med Chem. 2021 Oct 14;64(19):14773-14792. doi: 10.1021/acs.jmedchem.1c01356. Epub 2021 Oct 6. J Med Chem. 2021. PMID: 34613725
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Moore F, Wang W, Zhao G, Mignone J, Meng W, Chu CH, Ma Z, Azzara A, Cullen MJ, Pelleymounter MA, Appiah K, Cvijic ME, Dierks E, Chang S, Foster K, Kopcho L, O'Malley K, Li YX, Khandelwal P, Whaley JM, Mathur A, Hou X, Wu DR, Robl JA, Cheng D, Devasthale P. Moore F, et al. Among authors: devasthale p. Bioorg Med Chem Lett. 2023 Jul 15;91:129362. doi: 10.1016/j.bmcl.2023.129362. Epub 2023 Jun 8. Bioorg Med Chem Lett. 2023. PMID: 37295614
Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders.
Meng W, Brigance R, Mignone J, Negash L, Zhao G, Ahmad S, Wang W, Moore F, Ye XY, Sun JH, Mathur A, Li YX, Azzara A, Ma Z, Chu CH, Cullen MJ, Rooney S, Harvey S, Kopcho L, Abell L, O'Malley K, Keim W, Dierks EA, Chang S, Foster KA, Harden D, Dabros M, Goti V, De Oliveira C, Krishna G, Pelleymounter MA, Whaley J, Robl JA, Cheng D, Devasthale P. Meng W, et al. Among authors: devasthale p. J Med Chem. 2023 Sep 28;66(18):13135-13147. doi: 10.1021/acs.jmedchem.3c01147. Epub 2023 Sep 19. J Med Chem. 2023. PMID: 37724542
Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.
Washburn WN, Manfredi M, Devasthale P, Zhao G, Ahmad S, Hernandez A, Robl JA, Wang W, Mignone J, Wang Z, Ngu K, Pelleymounter MA, Longhi D, Zhao R, Wang B, Huang N, Flynn N, Azzara AV, Barrish JC, Rohrbach K, Devenny JJ, Rooney S, Thomas M, Glick S, Godonis HE, Harvey SJ, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Maxwell BD, Yang H, Apedo A, Gemzik B, Janovitz EB, Huang C, Zhang L, Freeden C, Murphy BJ. Washburn WN, et al. Among authors: devasthale p. J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9. J Med Chem. 2014. PMID: 25165888
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Devasthale PV, Chen S, Jeon Y, Qu F, Ryono DE, Wang W, Zhang H, Cheng L, Farrelly D, Golla R, Grover G, Ma Z, Moore L, Seethala R, Sun W, Doweyko AM, Chandrasena G, Sleph P, Hariharan N, Cheng PT. Devasthale PV, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2312-6. doi: 10.1016/j.bmcl.2007.01.060. Epub 2007 Jan 25. Bioorg Med Chem Lett. 2007. PMID: 17292606
22 results