The design of non-peptide human Bradykinin B-12 receptor antagonists employing the benzodiazepine peptidomimetic scaffold

Authors
Dziadulewicz, EK Brown, MC Dunstan, AR Lee, W Said, NB Garratt, PJ
Citation
Ek. Dziadulewicz et al., The design of non-peptide human Bradykinin B-12 receptor antagonists employing the benzodiazepine peptidomimetic scaffold, BIOORG MED, 9(3), 1999, pp. 463-468
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
3
Year of publication
1999
Pages
463 - 468
Database
ISI
SICI code
0960-894X(19990208)9:3<463:TDONHB>2.0.ZU;2-3
Abstract
The Bradykinin B-2 receptor antagonist HOE 140 (D-Arg-Arg-Pro-EIyp-Gly-Thi- Ser-D-Tic-Oic-Arg) has been used as a template for the de novo design and s ynthesis of a small number of non-peptide lead compounds based on the 1,4-b enzodiazepin-2-one framework. Two of the compounds have been found to exhib it moderate K-i values of 8.9 and 9.2 mu M at the human Bradykinin B-2 rece ptor. (C) 1999 Elsevier Science Ltd. All rights reserved.