Rational design of a pirinixic acid derivative that acts as subtype-selective PPARγ modulator

…, A Paulke, G Schneider, M Schubert-Zsilavecz

Index: Thieme, Theresa M.; Steri, Ramona; Proschak, Ewgenij; Paulke, Alexander; Schneider, Gisbert; Schubert-Zsilavecz, Manfred Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2469 - 2473

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Citation Number: 12

Abstract

Peroxisome proliferator-activated receptor γ (PPARγ) is involved in glucose and lipid homeostasis. PPARγ agonists are in clinical use for the treatment of type 2 diabetes. Lately, a new class of selective PPARγ modulators (SPPARγMs) was developed, which are believed to show less side effects than full PPARγ agonists. We have previously shown that α-substitution of pirinixic acid, a moderate agonist of PPARα and PPARγ, leads to low ...