Non-peptidic phenyl-based thrombin inhibitors: Exploring structural requirements of the S1 specificity pocket with amidines

Authors
Lu, TB Tomczuk, B Bone, R Murphy, L Salemme, FR Soll, RM
Citation
Tb. Lu et al., Non-peptidic phenyl-based thrombin inhibitors: Exploring structural requirements of the S1 specificity pocket with amidines, BIOORG MED, 10(1), 2000, pp. 83-85
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
1
Year of publication
2000
Pages
83 - 85
Database
ISI
SICI code
0960-894X(20000103)10:1<83:NPTIES>2.0.ZU;2-M
Abstract
We expand the structural requirements and structure-activity relationship o f a novel class of non-peptidic aryl-based thrombin inhibitors through expl oration of the S1 specificity pocket of thrombin using flexible and constra ined amidines. The most active compound of this class is 11 with K-i = 69 n M, which is ca. 15-fold less potent than constrained guanidine 5. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.