412007-81-9Relevant academic research and scientific papers
Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-γ binding agents with potential application to the treatment of osteoporosis
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.
, p. 5659 - 5663 (2007/10/03)
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 = 50 nM) as a potent binding agent of PPAR-γ. Also reported is preliminary cell based data suggesting the use of these compounds in the treatment of osteoporosis.
