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ID: ALA2034891
Journal: Eur J Med Chem
Title: Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo.
Authors: Ham J, Hwang H, Kim E, Kim JA, Cho SJ, Ko J, Lee W, Lee J, Holla H, Banerjee J, Kim S, Yang I, Lee HJ, Shin K, Choi H, Nam SJ, Tak J, Hahn D, Oh T, Won DH, Lee TG, Choi J, Park MS, Seok C, Chin J, Kang H.
Abstract: We have discovered and demonstrated the in vitro and in vivo PPARδ-selective activity of novel Y-shaped agonists. These compounds activated hPPARδ with EC(50) values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARδ agonists with 10(4)-fold selectivity over the other two subtypes, namely, hPPARα and hPPARγ. The PPARδ ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy.
CiteXplore: 22534184