Structural comparison between type I and type II antagonists: Possible implications in the drug design of AT1 antagonists

Authors
Roumelioti, P Tselios, T Alexopoulos, K Mavromoustakos, T Kolocouris, A Moore, GJ Matsoukas, JM
Citation
P. Roumelioti et al., Structural comparison between type I and type II antagonists: Possible implications in the drug design of AT1 antagonists, BIOORG MED, 10(8), 2000, pp. 755-758
Citations number
10
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
8
Year of publication
2000
Pages
755 - 758
Database
ISI
SICI code
0960-894X(20000417)10:8<755:SCBTIA>2.0.ZU;2-3
Abstract
Analogues of sarilesin (type I AT1 antagonists), and sarmesin (type II AT1 antagonists) with homoserine (hSer) at position 8 were prepared and bioassa yed. The presence of a Tyr(4)-Ile(5)-His(6) bend found in sarmesin but not in sarilesin was identified. The obtained results coupled with conformation al analysis studies, using a combination of NMR spectroscopy and computatio nal chemistry, propose important conformational and stereoelectronic proper ties for agonist and antagonist activity at ATI receptors. (C) 2000 Elsevie r Science Ltd. All rights reserved.