Tryptophan-containing dipeptide derivatives as potent PPARγ antagonists: design, synthesis, biological evaluation, and molecular modeling

G Deng, Z Liu, F Ye, X Luo, W Zhu, X Shen…

Index: Deng, Guanghui; Liu, Zhiguo; Ye, Fei; Luo, Xiaomin; Zhu, Weiliang; Shen, Xu; Liu, Hong; Jiang, Hualiang European Journal of Medicinal Chemistry, 2008 , vol. 43, # 12 p. 2699 - 2716

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Citation Number: 11

Abstract

The discovery of peroxisome proliferator-activated receptor γ (PPARγ) antagonists (also termed “selective PPARγ modulators, SPPARγM”) is now of a great interest in the treatment of diabetes and obesity. The structure of compound 1a (G3335, Fig. 1), a novel class of PPARγ antagonist, is entirely different from that of other reported PPARγ antagonists. A series of 35 novel analogues (1b–l, 9a–d, 13a–t) were designed, synthesized and ...