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A novel class of oral direct renin inhibitors - highly potent 3,5-disubstituted piperidines bearing a tricyclic P3-P1 unit

Ostermann, Nils and Ruedisser, Simon and Ehrhardt, Claus and Breitenstein, Werner and Marzinzik, Andreas and Jacoby, Edgar and Vangrevelinghe, Eric and Ottl, Johannes and Klumpp, Martin and Mueller-Hartwieg, Constanze and Cumin, Frederic and Hassiepen, Ulrich and Trappe, Joerg and Geisse, Sabine and Gerhartz, Bernd and Richert, Paul and Francotte, Eric and Wagner, Beatrix and Kosaka, Takatoshi and Webb, Randy and Maibaum, Juergen Klaus and Baeschlin, Daniel and Sedrani, Richard (2013) A novel class of oral direct renin inhibitors - highly potent 3,5-disubstituted piperidines bearing a tricyclic P3-P1 unit. Journal of medicinal chemistry, 56 (6). pp. 2196-2206. ISSN 0022-2623

Abstract

The design and synthesis of a new direct renin inhibitor chemotype based on a 3,5-disubstituted piperidine bearing a tricyclic P3-P1 unit (4, IC50: 4 nM) is described. It is derived from a high-throughput screening hit containing the 3,5-disubstituted piperidine (3, IC50: 1.2 uM) and a tricyclic fragment (2, IC50 >100 uM) binding to the S1-S3 site of renin.

Item Type: Article
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16
URI: https://oak.novartis.com/id/eprint/2184

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