| Literature DB >> 22608962 |
William McCoull1, Matthew S Addie, Alan M Birch, Susan Birtles, Linda K Buckett, Roger J Butlin, Suzanne S Bowker, Scott Boyd, Stephen Chapman, Robert D M Davies, Craig S Donald, Clive P Green, Chloe Jenner, Paul D Kemmitt, Andrew G Leach, Graeme C Moody, Pablo Morentin Gutierrez, Nicholas J Newcombe, Thorsten Nowak, Martin J Packer, Alleyn T Plowright, John Revill, Paul Schofield, Chris Sheldon, Steve Stokes, Andrew V Turnbull, Steven J Y Wang, David P Whalley, J Matthew Wood.
Abstract
A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid containing clinical candidate 53 (AZD3988), which demonstrated excellent DGAT-1 potency (0.6 nM), good pharmacokinetics and pre-clinical in vivo efficacy that could be rationalised through a PK/PD relationship.Entities:
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Year: 2012 PMID： 22608962 DOI： 10.1016/j.bmcl.2012.04.117
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823