Piperidine-renin inhibitors compounds with improved physicochemical properties

Authors
Guller, R Binggeli, A Breu, V Bur, D Fischli, W Hirth, G Jenny, C Kansy, M Montavon, F Muller, M Oefner, C Stadler, H Vieira, E Wilhelm, M Wostl, W Marki, HP
Citation
R. Guller et al., Piperidine-renin inhibitors compounds with improved physicochemical properties, BIOORG MED, 9(10), 1999, pp. 1403-1408
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
10
Year of publication
1999
Pages
1403 - 1408
Database
ISI
SICI code
0960-894X(19990517)9:10<1403:PICWIP>2.0.ZU;2-I
Abstract
Piperidine renin inhibitors with heterocyclic core modifications or hydroph ilic attachments show improved physical properties (lower lipophilicity, im proved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting b lood pressure lowering effects after oral administration to sodium depleted conscious marmosets. (C) 1999 Elsevier Science Ltd. All rights reserved.