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

  • Bioorg Med Chem Lett. 1998 Mar 17;8(6):631-4. doi: 10.1016/s0960-894x(98)00079-1.
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
  • 1. Biotech Research Institute, LG Chemical LTD, Taejon, Korea.
PMID: 9871573 DOI: 10.1016/s0960-894x(98)00079-1
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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