Development of tryptase inhibitors derived from thalidomide

Masashi Tetsuhashi, Minoru Ishikawa, Mariko Hashimoto, Yuichi Hashimoto, Hiroshi Aoyama

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)

Abstract

A novel series of tryptase inhibitors with a N-phenylphthalimide skeleton structurally derived from thalidomide (1) has been developed. Structure-activity relationship studies led to a potent and selective tryptase inhibitor, 2-(4-cyanophenyl)isoindole-1,3-dione-5-yl 3-(2-aminopyridin-5-yl)propanoate (7), with the IC 50 value of 78 nM.

Original languageEnglish
Pages (from-to)5323-5338
Number of pages16
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number14
DOIs
Publication statusPublished - 2010 Jul 15
Externally publishedYes

Keywords

  • Inhibitor
  • Phthalimide
  • Serine protease
  • Thalidomide
  • Tryptase

ASJC Scopus subject areas

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

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