Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
, 21 (8), 2541-6

Design, Synthesis and Structure-Activity Relationships of (indo-3-yl) Heterocyclic Derivatives as Agonists of the CB1 Receptor. Discovery of a Clinical Candidate

Affiliations

Design, Synthesis and Structure-Activity Relationships of (indo-3-yl) Heterocyclic Derivatives as Agonists of the CB1 Receptor. Discovery of a Clinical Candidate

Paul Ratcliffe et al. Bioorg Med Chem Lett.

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.

Similar articles

See all similar articles

LinkOut - more resources

Feedback