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Page 1
Diaminoindanes as microsomal triglyceride transfer protein inhibitors.
Ksander GM, deJesus R, Yuan A, Fink C, Moskal M, Carlson E, Kukkola P, Bilci N, Wallace E, Neubert A, Feldman D, Mogelesky T, Poirier K, Jeune M, Steele R, Wasvery J, Stephan Z, Cahill E, Webb R, Navarrete A, Lee W, Gibson J, Alexander N, Sharif H, Hospattankar A. Ksander GM, et al. J Med Chem. 2001 Dec 20;44(26):4677-87. doi: 10.1021/jm010294e. J Med Chem. 2001. PMID: 11741485
Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans.
Nakajima K, Chatelain R, Clairmont KB, Commerford R, Coppola GM, Daniels T, Forster CJ, Gilmore TA, Gong Y, Jain M, Kanter A, Kwak Y, Li J, Meyers CD, Neubert AD, Szklennik P, Tedesco V, Thompson J, Truong D, Yang Q, Hubbard BK, Serrano-Wu MH. Nakajima K, et al. Among authors: neubert ad. J Med Chem. 2017 Jun 8;60(11):4657-4664. doi: 10.1021/acs.jmedchem.7b00173. Epub 2017 May 24. J Med Chem. 2017. PMID: 28498655 Clinical Trial.
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Kawanami T, Karki RG, Cody E, Liu Q, Liang G, Ksander GM, Rigel DF, Schiering N, Gong Y, Coppola GM, Iwaki Y, Sun R, Neubert A, Fan L, Ingles S, D'Arcy A, Villard F, Ramage P, Jeng AY, Leung-Chu J, Liu J, Beil M, Fu F, Chen W, Cumin F, Wiesmann C, Mogi M. Kawanami T, et al. ACS Med Chem Lett. 2020 Jan 27;11(2):188-194. doi: 10.1021/acsmedchemlett.9b00578. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071687 Free PMC article.
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.
Serrano-Wu MH, Coppola GM, Gong Y, Neubert AD, Chatelain R, Clairmont KB, Commerford R, Cosker T, Daniels T, Hou Y, Jain M, Juedes M, Li L, Mullarkey T, Rocheford E, Sung MJ, Tyler A, Yang Q, Yoon T, Hubbard BK. Serrano-Wu MH, et al. Among authors: neubert ad. ACS Med Chem Lett. 2012 Apr 4;3(5):411-5. doi: 10.1021/ml3000512. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900485 Free PMC article.
A new structural alert for benzimidazoles: 2,6-dimethylphenyl substituents increase mutagenic potential and time-dependent CYP3A4 inhibition risk.
Kwak Y, Coppola G, Forster CJ, Gilmore TA, Gong Y, Kanter A, Neubert A, Stroup B, Szklennik P, Glowienke S, Stadelmann P, Bell L, Bickford S, Gangl E, Gunduz M, Jain M, Zhan J, Serrano-Wu MH. Kwak Y, et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1422-4. doi: 10.1016/j.bmcl.2011.01.023. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295471