新型N-磺酰基-2-吲哚甲酰胺的设计与合成：作为有效的PPAR-γ结合剂及其在骨质疏松症治疗中的潜在应用
Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.
作者信息
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 Thomas P
机构信息
Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason OH 45040, USA.
出版信息
Bioorg Med Chem Lett. 2006 Nov 1;16(21):5659-63. doi: 10.1016/j.bmcl.2006.08.003. Epub 2006 Aug 21.
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-gamma) are reported. Chemical optimization of the series led to the identification of 4q (IC(50)=50 nM) as a potent binding agent of PPAR-gamma. Also reported is preliminary cell based data suggesting the use of these compounds in the treatment of osteoporosis.
报道了一系列与过氧化物酶体增殖物激活受体γ（PPAR-γ）结合的新型N-磺酰基-2-吲哚甲酰胺的合成及其构效关系。对该系列化合物进行化学优化后，确定4q（IC50 = 50 nM）为PPAR-γ的有效结合剂。还报道了基于细胞的初步数据，表明这些化合物可用于治疗骨质疏松症。
Zotero 插件