| Autor: |
Filzen GF; Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. Gary.filzen@pfizer.com , Bratton L, Cheng XM, Erasga N, Geyer A, Lee C, Lu G, Pulaski J, Sorenson RJ, Unangst PC, Trivedi BK, Xu X |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jul 01; Vol. 17 (13), pp. 3630-5. Date of Electronic Publication: 2007 Apr 24. |
| DOI: |
10.1016/j.bmcl.2007.04.047 |
| Abstrakt: |
Recent literature has suggested the benefit of selective PPARdelta agonists for the treatment of atherosclerosis and other disease states associated with the metabolic syndrome. Herein we report the synthesis and structure-activity relationships of a series of novel and selective PPARdelta agonists. Our search began with identification of a novel benzothiophene template which was modified by the addition of various thiazolyl, isoxazolyl, and benzyloxy-benzyl moieties. Further elucidation of the SAR led to the identification of benzofuran and indole based templates. During the course of our research, we discovered three new chemical templates with varying degrees of affinity and potency for PPARdelta versus the PPARalpha and PPARgamma subtypes. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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