32835-74-8Relevant academic research and scientific papers
Discovery of a peroxisome proliferator activated receptor γ (PPARγ) modulator with balanced PPARα activity for the treatment of type 2 diabetes and dyslipidemia
Liu, Weiguo,Liu, Kun,Wood, Harold B.,McCann, Margaret E.,Doebber, Thomas W.,Chang, Ching H.,Akiyama, Taro E.,Einstein, Monica,Berger, Joel P.,Meinke, Peter T.
supporting information; experimental part, p. 4443 - 4453 (2010/03/02)
A series of 3-acylindole-1-benzylcarboxylic acids were designed and synthesized while searching for a PPARγ modulator with additional moderate intrinsic PPARα agonistic activity. 2-[3-[[3-(4-Chlorobenzoyl)-2-methyl- 6-(trifluoromethoxy)-1H-indol-1-yl]methyl]phenoxy]-(2R)-butanoic acid (12d) was identified as such an agent which demonstrated potent efficacy in lowering both glucose and lipids in multiple animal models with significantly attenuated side effects such as fluid retention and heart weight gain associated with PPARγ full agonists. The moderate PPARα activity of 12d not only contributed to the agent's ability to manage lipid profiles but also appears to have potentiated its PPARγ efficacy in lowering glucose levels in preclinical diabetic animal models.
Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1
Fink, Cynthia A.,Moskal, Michael,Firooznia, Fariborz,Hoyer, Denton,Symonsbergen, David,Wei, Dongchu,Qiao, Ying,Savage, Paula,Beil, Michael E.,Trapani, Angelo J.,Jeng, Arco Y.
, p. 2037 - 2039 (2007/10/03)
Through directed screening of compounds prepared as metalloprotease inhibitors a compound, CGS 30084, that had potent endothelin converting enzyme-1 (ECE-1) in vitro inhibitory activity (IC50=77nM) was identified. Herein we report the synthesis and optimization of ECE-1 inhibitory activity of additional analogues from this lead. Compound 3c, the thioacetate methyl ester derivative of compound 4c, was found to be a long acting inhibitor of ECE-1 activity in rats after oral administration. (C) 2000 Elsevier Science Ltd.
Asymmetric Synthesis of 2-Chloro- and 2-Bromo-alkanoic acids by Halogenation of α-D-Glucofuranose-Derived Silyl Ketene Acetals.
Angibaud, P.,Chaumette, J. L.,Desmurs, J. R.,Duhamel, L.,Ple, G.,et al.
, p. 1919 - 1932 (2007/10/03)
Optically active (S)-2-bromo- and 2-chloro-alkanoic acids 6 and 7 have been obtained via the diastereoselective halogenation of chiral silyl ketene acetals 3a-f, and subsequent saponification of the resulting crude esters.Examples characterized by e.e. values up to 95percent are reported.The diastereoface selectivity is independent of the silyl ketene acetal E/Z configuration.
