892489-13-3Relevant articles and documents
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes
McCoull, William,Addie, Matthew S.,Birch, Alan M.,Birtles, Susan,Buckett, Linda K.,Butlin, Roger J.,Bowker, Suzanne S.,Boyd, Scott,Chapman, Stephen,Davies, Robert D.M.,Donald, Craig S.,Green, Clive P.,Jenner, Chloe,Kemmitt, Paul D.,Leach, Andrew G.,Moody, Graeme C.,Morentin Gutierrez, Pablo,Newcombe, Nicholas J.,Nowak, Thorsten,Packer, Martin J.,Plowright, Alleyn T.,Revill, John,Schofield, Paul,Sheldon, Chris,Stokes, Steve,Turnbull, Andrew V.,Wang, Steven J.Y.,Whalley, David P.,Matthew Wood
, p. 3873 - 3878 (2012/07/03)
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), wh