1.
Bioorg Med Chem Lett
; 21(8): 2541-6, 2011 Apr 15.
Article
in English
| MEDLINE
| ID: mdl-21411321
ABSTRACT
We report an expansion of the structure-activity relationship (SAR) of a novel series of indole-3-heterocyclic CB1 receptor agonists. Starting from the potent but poorly soluble lead, 1, a rational approach was taken in order to balance solubility, hERG activity and potency while retaining the desired long duration of action within the mouse tail flick test. This led to the discovery of compound 38 which successfully progressed into clinical development.