✦ LIBER ✦

ChemInform Abstract: Modulation of PPAR Subtype Selectivity. Part 2. Transforming PPARα/γ Dual Agonist into α Selective PPAR Agonist Through Bioisosteric Modification.

✍ Scribed by Rajesh Bahekar; et al. et al.

Publisher: John Wiley and Sons
Year: 2011
Weight: 25 KB
Volume: 42
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.201121200

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✦ Synopsis

Bioisosteric replacement of the rigid oxazole ring of a previously reported PPARα/γ dual agonist with a flexible lipophilic tail leads to a series of oxime containing benzyl dioxanecarboxylic acid derivatives. Compounds (I) show high selectivity towards PPARα over PPARγ in vitro. Furthermore, the highly potent and selective PPARα agonist (Ic) exerts significant antihyperglycemic and antihyperlipidemic activity in vivo, along with an improved pharmacokinetic profile. Favorable in-silico interaction of (Ic) with PPARα binding pocket and partial interaction with PPARγ binding pocket correlates its in vitro selectivity profile.

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