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Page 1
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: minich ml. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.
Pfefferkorn JA, Lou J, Minich ML, Filipski KJ, He M, Zhou R, Ahmed S, Benbow J, Perez AG, Tu M, Litchfield J, Sharma R, Metzler K, Bourbonais F, Huang C, Beebe DA, Oates PJ. Pfefferkorn JA, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3247-52. doi: 10.1016/j.bmcl.2009.04.107. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19435665
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y. Darout E, et al. Among authors: minich ml. J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31. J Med Chem. 2013. PMID: 23234271
Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2.
Corbett JW, Freeman-Cook KD, Elliott R, Vajdos F, Rajamohan F, Kohls D, Marr E, Zhang H, Tong L, Tu M, Murdande S, Doran SD, Houser JA, Song W, Jones CJ, Coffey SB, Buzon L, Minich ML, Dirico KJ, Tapley S, McPherson RK, Sugarman E, Harwood HJ Jr, Esler W. Corbett JW, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2383-8. doi: 10.1016/j.bmcl.2009.04.091. Epub 2009 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20219367
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
Cheng H, Lundy DeMello KM, Li J, Sakya SM, Ando K, Kawamura K, Kato T, Rafka RJ, Jaynes BH, Ziegler CB, Stevens R, Lund LA, Mann DW, Kilroy C, Haven ML, Nimz EL, Dutra JK, Li C, Minich ML, Kolosko NL, Petras C, Silvia AM, Seibel SB. Cheng H, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2076-80. doi: 10.1016/j.bmcl.2006.01.059. Epub 2006 Feb 7. Bioorg Med Chem Lett. 2006. PMID: 16464588
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
Robinson RP, Bartlett JA, Bertinato P, Bessire AJ, Cosgrove J, Foley PM, Manion TB, Minich ML, Ramos B, Reese MR, Schmahai TJ, Swick AG, Tess DA, Vaz A, Wolford A. Robinson RP, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4. doi: 10.1016/j.bmcl.2011.05.099. Epub 2011 Jun 2. Bioorg Med Chem Lett. 2011. PMID: 21684740
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Li J, DeMello KM, Cheng H, Sakya SM, Bronk BS, Rafka RJ, Jaynes BH, Ziegler CB, Kilroy C, Mann DW, Nimz EL, Lynch MP, Haven ML, Kolosko NL, Minich ML, Li C, Dutra JK, Rast B, Crosson RM, Morton BJ, Kirk GW, Callaghan KM, Koss DA, Shavnya A, Lund LA, Seibel SB, Petras CF, Silvia A. Li J, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2004 Jan 5;14(1):95-8. doi: 10.1016/j.bmcl.2003.10.004. Bioorg Med Chem Lett. 2004. PMID: 14684306
5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.
Sakya SM, DeMello KM, Minich ML, Rast B, Shavnya A, Rafka RJ, Koss DA, Cheng H, Li J, Jaynes BH, Ziegler CB, Mann DW, Petras CF, Seibel SB, Silvia AM, George DM, Lund LA, St Denis S, Hickman A, Haven ML, Lynch MP. Sakya SM, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2006 Jan 15;16(2):288-92. doi: 10.1016/j.bmcl.2005.10.006. Epub 2005 Nov 3. Bioorg Med Chem Lett. 2006. PMID: 16275075
5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.
Sakya SM, Cheng H, Lundy Demello KM, Shavnya A, Minich ML, Rast B, Dutra J, Li C, Rafka RJ, Koss DA, Li J, Jaynes BH, Ziegler CB, Mann DW, Petras CF, Seibel SB, Silvia AM, George DM, Hickman A, Haven ML, Lynch MP. Sakya SM, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1202-6. doi: 10.1016/j.bmcl.2005.11.110. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16380252
5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile.
Sakya SM, Hou X, Minich ML, Rast B, Shavnya A, DeMello KM, Cheng H, Li J, Jaynes BH, Mann DW, Petras CF, Seibel SB, Haven ML. Sakya SM, et al. Among authors: minich ml. Bioorg Med Chem Lett. 2007 Feb 15;17(4):1067-72. doi: 10.1016/j.bmcl.2006.11.026. Epub 2006 Nov 15. Bioorg Med Chem Lett. 2007. PMID: 17126015
12 results