Ostermann, Nils, Ruedisser, Simon, Ehrhardt, Claus, Breitenstein, Werner, Marzinzik, Andreas, Jacoby, Edgar, Vangrevelinghe, Eric, Ottl, Johannes, Klumpp, Martin, Mueller-Hartwieg, Constanze, Cumin, Frederic, Hassiepen, Ulrich, Trappe, Joerg, Geisse, Sabine, Gerhartz, Bernd, Richert, Paul, Francotte, Eric, Wagner, Beatrix, Kosaka, Takatoshi, Webb, Randy, Maibaum, Juergen Klaus, 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
Related URLs:	http://www.ncbi.nlm.nih.gov/pubmed/?term...
Related URLs:	http://www.ncbi.nlm.nih.gov/pubmed/?term...
Date Deposited:	13 Oct 2015 13:16
Last Modified:	13 Oct 2015 13:16
URI:	https://oak.novartis.com/id/eprint/2184