129644-21-9Relevant articles and documents
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
Walsh, Shawn P.,Severino, Alexandra,Zhou, Changyou,He, Jiafang,Liang, Gui-Bai,Tan, Carina P.,Cao, Jin,Eiermann, George J.,Xu, Ling,Salituro, Gino,Howard, Andrew D.,Mills, Sander G.,Yang, Lihu
scheme or table, p. 3390 - 3394 (2011/06/24)
The design, synthesis, and structure-activity relationship (SAR) for a series of β-substituted 3-(4-aryloxyaryl)propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, serum shifted potency and pharmacokinetic properties were determined for several compounds. Finally, further profiling of compound 7 is presented, including demonstration of enhanced glucose tolerance in an in vivo mouse model.
Simple preparation of 4-aryl- and 4-alkyl-2(5H)-furanones from β-substituted crotonic esters
Kagabu,Shimizu,Ito,Moriya
, p. 830 - 832 (2007/10/02)
Treatment of β-aryl- or β-alkylcrotonic esters with selenium dioxide in acetic acid in the presence of a catalytic amount of perchloric acid gave 4-substituted 2(5H)-furanones in moderate to good yields.
