BIARYL SUBSTITUTED ALKYLBORONATE ESTERS AS THROMBIN INHIBITORS

Authors
QUAN ML WITYAK J DOMINGUEZ C DUNCIA JV KETTNER CA ELLIS CD LIAUW AY PARK JM SANTELLA JB KNABB RM THOOLEN MJ WEBER PC WEXLER RR
Citation
Ml. Quan et al., BIARYL SUBSTITUTED ALKYLBORONATE ESTERS AS THROMBIN INHIBITORS, Bioorganic & medicinal chemistry letters, 7(13), 1997, pp. 1595-1600
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
13
Year of publication
1997
Pages
1595 - 1600
Database
ISI
SICI code
0960-894X(1997)7:13<1595:BSAEAT>2.0.ZU;2-Y
Abstract
Thrombin is a serine protease that plays an important role in the bloo d coagulation cascade, and is a target enzyme for new therapeutic agen ts. Ac-(D)-Phe-Pro-boroArg-OH (DuP714) was found to be a highly effect ive thrombin inhibitor. In order to reduce the peptidic nature of DuP 714, we have designed a series of novel biaryl substituted alkylborona te esters as potent thrombin inhibitors. The most potent compounds hav e subnanomolar affinity for thrombin. (C) 1997 The DuPont Merck Pharma ceutical Company. Published by Elsevier Science Ltd.