| Literature DB >> 30952592 |
Yang Yu1, Zhicai Wu2, Zhi-Cai Shi2, Shuwen He2, Zhong Lai2, Timothy A Cernak2, Petr Vachal2, Min Liu2, Jian Liu2, Qingmei Hong2, Tianying Jian2, Deodial Guiadeen2, Arto Krikorian2, Donald M Sperbeck2, Andreas Verras2, Lisa M Sonatore2, Beth A Murphy2, Judyann Wiltsie2, Christine C Chung2, Judith N Gorski2, Jinqi Liu2, Jianying Xiao2, Michael Wolff2, Sharon X Tong2, Maria Madeira2, Bindhu V Karanam2, Dong-Ming Shen2, James M Balkovec2, Robert J De Vita2, Shirly Pinto2, Ravi P Nargund2.
Abstract
The parallel medicinal chemistry (PMC) was effectively applied to accelerate the optimization of diacylglycerol O-acyltransferase I (DGAT-1) inhibitors. Through a highly collaborative and iterative library design, synthesis and testing, a benzimidazole lead was rapidly and systematically advanced to a highly potent, selective and bioavailable DGAT1 inhibitor with the potential for further development.Entities:
Keywords: A(2A) receptor; ACAT1; Benzimidazole; Cyclohexane acetic acid; DGAT1 inhibitor; High throughput purification; Lipid tolerance test; Parallel medicinal chemistry; Pharmacokinetics; Triglyceride
Year: 2019 PMID： 30952592 DOI： 10.1016/j.bmcl.2019.03.039
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823