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 journalArticlepeer-review

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)4281-4286
Number of pages6
JournalBioorganic & medicinal chemistry letters
Volume14
Issue number16
Publication statusPublished - 2004 Aug 16

ASJC Scopus subject areas

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

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