DISCOVERY OF LB30057, A BENZAMIDRAZONE-BASED SELECTIVE ORAL THROMBIN INHIBITOR

Authors
OH YS YUN M HWANG SY HONG S SHIN Y LEE K YOON KH YOO YJ KIM DS LEE SH LEE YH PARK HD LEE CH LEE SK KIM S
Citation
Ys. Oh et al., DISCOVERY OF LB30057, A BENZAMIDRAZONE-BASED SELECTIVE ORAL THROMBIN INHIBITOR, Bioorganic & medicinal chemistry letters, 8(6), 1998, pp. 631-634
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
6
Year of publication
1998
Pages
631 - 634
Database
ISI
SICI code
0960-894X(1998)8:6<631:DOLABS>2.0.ZU;2-1
Abstract
Systematic variation of the so-called P-pocket moiety of benzamidrazon e-based selective thrombin inhibitors led to the discovery of LB30057. It is potent (Ki = 0.38 nM for human thrombin), selective (Ki = 3290 nM for bovine trypsin), and orally bioavailable (58% oral bioavailabil ity in dogs). LB30057 was efficacious in thrombosis animal models. (C) 1998 Elsevier Science Ltd. All rights reserved.