| Literature DB >> 20219367 |
Jeffrey W Corbett1, Kevin D Freeman-Cook, Richard Elliott, Felix Vajdos, Francis Rajamohan, Darcy Kohls, Eric Marr, Hailong Zhang, Liang Tong, Meihua Tu, Sharad Murdande, Shawn D Doran, Janet A Houser, Wei Song, Christopher J Jones, Steven B Coffey, Leanne Buzon, Martha L Minich, Kenneth J Dirico, Susan Tapley, R Kirk McPherson, Eliot Sugarman, H James Harwood, William Esler.
Abstract
Screening Pfizer's compound library resulted in the identification of weak acetyl-CoA carboxylase inhibitors, from which were obtained rACC1 CT-domain co-crystal structures. Utilizing HTS hits and structure-based drug discovery, a more rigid inhibitor was designed and led to the discovery of sub-micromolar, spirochromanone non-specific ACC inhibitors. Low nanomolar, non-specific ACC-isozyme inhibitors that exhibited good rat pharmacokinetics were obtained from this chemotype. 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20219367 DOI： 10.1016/j.bmcl.2009.04.091
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823