Synthesis of annulated pyridines as inhibitors of aldosterone synthase (CYP11B2)?

Organic & Biomolecular Chemistry Pub Date: 2016-06-01 DOI: 10.1039/C6OB00848H

Abstract

A series of cyclopenta[c]pyridine aldosterone synthase (AS) inhibitors were conveniently accessed using batch or continuous flow Kondrat'eva reactions. Preparation of the analogous cyclohexa[c]pyridines led to the identification of a potent and more selective AS inhibitor. The structure-activity-relationship (SAR) in this new series was rationalized using binding mode models in the crystal structure of AS.

Graphical abstract: Synthesis of annulated pyridines as inhibitors of aldosterone synthase (CYP11B2)
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