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Bioorg Med Chem Lett. 2010 Aug 1;20(15):4573-7. doi: 10.1016/j.bmcl.2010.06.017. Epub 2010 Jun 8.

Rational design of a novel peripherally-restricted, orally active CB(1) cannabinoid antagonist containing a 2,3-diarylpyrrole motif.

Author information

1
Exploratory Unit, Sanofi-aventis R&D, 371 rue du Professeur Joseph Blayac, Montpellier, France.

Abstract

A new series of 2,3-diarylpyrroles have been prepared and evaluated as CB(1) antagonists. Modulation of the topological polar surface area allowed the identification of high affinity peripherally-restricted CB(1) antagonists. Compound 11, obtained after further optimization of the metabolic profile displayed very low brain penetration, yet was able to reverse CP55940-induced gastrointestinal transit inhibition following oral administration.

PMID:
20584609
DOI:
10.1016/j.bmcl.2010.06.017
[Indexed for MEDLINE]

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