Author/Authors :
Corey R. Hopkins، نويسنده , , Steven V. O’Neil، نويسنده , , Michael C. Laufersweiler، نويسنده , , Yili Wang، نويسنده , , Matthew Pokross، نويسنده , , Marlene Mekel، نويسنده , , Artem Evdokimov، نويسنده , , Richard Walter، نويسنده , , Maria Kontoyianni، نويسنده , , Maria E. Petrey، نويسنده , , Georgios Sabatakos، نويسنده , , Jeff T. Roesgen، نويسنده , , Eloise Richardson، نويسنده , , Thomas P. Demuth Jr.، نويسنده ,
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 = 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.
Keywords :
Anti-HIV , structure-based drug design , 2-Pyrimidinylamine , Free energy perturbation , NNRTI , Triazinylamine
