The design and synthesis of thrombin inhibitors: Analogues of MD805 containing non-polar surrogates for arginine at the P1 position

Authors
Baettig, U Brown, L Brundish, D Dell, C Furzer, A Garman, S Janus, D Kane, PD Smith, G Walker, CV Cockcroft, XL Ambler, J Mitchelson, A Talbot, MD Tweed, M Wills, N
Citation
U. Baettig et al., The design and synthesis of thrombin inhibitors: Analogues of MD805 containing non-polar surrogates for arginine at the P1 position, BIOORG MED, 10(14), 2000, pp. 1563-1566
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
14
Year of publication
2000
Pages
1563 - 1566
Database
ISI
SICI code
0960-894X(20000717)10:14<1563:TDASOT>2.0.ZU;2-X
Abstract
A series of monocyclic and bicyclic amino acids have been synthesised and i ncorporated into thrombin inhibitors based on CGH728, an analogue of the Mi tsubishi compound MD805. Benzthiazolylalanine (Bta) was found to be a good non-polar substitute for arginine at the P1 position, yielding compounds wi th low nanomolar potency and good selectivity for thrombin. (C) 2000 Elsevi er Science Ltd. All rights reserved.