Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-γ binding agents with potential application to the treatment of osteoporosis

CR Hopkins, SV O'Neil, MC Laufersweiler…

Index: Hopkins, Corey R.; O'Neil, Steven V.; Laufersweiler, Michael C.; Wang, Yili; Pokross, Matthew; Mekel, Marlene; Evdokimov, Artem; Walter, Richard; Kontoyianni, Maria; Petrey, Maria E.; Sabatakos, Georgios; Roesgen, Jeff T.; Richardson, Eloise; Demuth Jr., Thomas P. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 21 p. 5659 - 5663

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Citation Number: 36

Abstract

The synthesis and structure–activity relationships of a novel series of N-sulfonyl-2-indole carboxamides that bind to peroxisome proliferator-activated receptor gamma (PPAR-γ) are reported. Chemical optimization of the series led to the identification of 4q (IC50= 50nM) ...