新型吲哚衍生物的合成及作为有效和选择性过氧化物酶体增殖物激活受体γ调节剂的生物活性。
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
机构信息
Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 Avenue du Québec, 91951 Les Ulis, France.
出版信息
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1399-404. doi: 10.1016/j.bmcl.2009.12.107. Epub 2010 Jan 4.
PMID:20079636
Abstract
Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds are reported and the X-ray structure of compound 7b bound to the PPARgamma ligand binding domain is described.
摘要
从替米沙坦的结构出发，我们鉴定出了一系列新的强效且选择性的过氧化物酶体增殖物激活受体γ调节剂。本文报道了其中最具活性化合物的合成、体外和体内评价结果，并描述了化合物 7b 与过氧化物酶体增殖物激活受体γ配体结合域结合的 X 射线结构。
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