Rational design of a novel peripherally-restricted, orally active CB1 cannabinoid antagonist containing a 2,3-diarylpyrrole motif
2010
A new series of 2,3-diarylpyrroles have been prepared and evaluated as CB1 antagonists. Modulation of the topological polar surface area allowed the identification of high affinity peripherally-restricted CB1 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.
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