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Bioorg Med Chem Lett. 1998 Mar 17;8(6):631-4.

Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.

Author information

1
Biotech Research Institute, LG Chemical LTD, Taejon, Korea.

Abstract

Systematic variation of the so-called P-pocket moiety of benzamidrazone-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 bioavailability in dogs). LB30057 was efficacious in thrombosis animal models.

PMID:
9871573
DOI:
10.1016/s0960-894x(98)00079-1
[Indexed for MEDLINE]

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