Title of article
Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-γ binding agents with potential application to the treatment of osteoporosis
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5659
To page
5663
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797450
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