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Issue 25, 2016
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Synthesis of annulated pyridines as inhibitors of aldosterone synthase (CYP11B2)

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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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Article information


Submitted
20 Apr 2016
Accepted
25 May 2016
First published
01 Jun 2016

Org. Biomol. Chem., 2016,14, 5922-5927
Article type
Communication

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

R. E. Martin, J. Lehmann, T. Alzieu, M. Lenz, M. A. Carnero Corrales, J. D. Aebi, H. P. Märki, B. Kuhn, K. Amrein, A. V. Mayweg and R. Britton, Org. Biomol. Chem., 2016, 14, 5922
DOI: 10.1039/C6OB00848H

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