Structure-activity relationships of potent and selective factor Xa inhibitors: Benzimidazole derivatives with the side chain oriented to the prime site of factor Xa

Hiroshi Ueno, Susumu Katoh, Katsuyuki Yokota, Jun Ichi Hoshi, Mikio Hayashi, Itsuo Uchida, Kazuo Aisaka, Yasunori Hase, Hidetsura Cho

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to the prime site of factor Xa (FXa) were designed and synthesized. Compounds with substituted aminocarbonylmethyl groups as the side chain showed potent FXa inhibitory activity. Compounds 1 and 2 exhibited most potent inhibitory activity and were effective as anticoagulants in a DIC model.

Original languageEnglish
Pages (from-to)4217-4220
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number16
DOIs
Publication statusPublished - 2004 Aug 16

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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