| Autor: |
Bratton LD; Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. ageyer1@gmail.com , Filzen GF, Geyer A, Hoffman JK, Lu G, Pulaski J, Trivedi BK, Unangst PC, Xu X |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jul 01; Vol. 17 (13), pp. 3624-9. Date of Electronic Publication: 2007 Apr 24. |
| DOI: |
10.1016/j.bmcl.2007.04.046 |
| Abstrakt: |
A series of 1,4-benzyloxybenzylsulfanylaryl carboxylic acids were prepared and their activities for PPAR receptor subtypes (alpha, delta, and gamma) with potential indications for the treatment of dyslipidemia were investigated. Analog 13a displayed the greatest binding affinity (IC(50)=10nM) and selectivity (120-fold) for PPARdelta over PPARalpha. Many of the analogs investigated were found to be highly selective for PPARdelta and were dependent on the point of attachment of the substituent. In the 1,4-series, analog 28e was found to be the most potent (IC(50)=1.7 nM) and selective (>1000-fold) compound for PPARdelta. None of the compounds tested showed appreciable binding affinity for PPARgamma. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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