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. 1998 Mar 17;8(6):631-4.
doi: 10.1016/s0960-894x(98)00079-1.

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

Y S Oh  1 , M Yun, S Y Hwang, S Hong, Y Shin, K Lee, K H Yoon, Y J Yoo, D S Kim, S H Lee, Y H Lee, H D Park, C H Lee, S K Lee, S Kim
Affiliations

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

Y S Oh et al. Bioorg Med Chem Lett. .

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.

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