Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

Hyunmin Song, Sei Ryang Oh, Hyeong Kyu Lee, Gyoonhee Han, Joo Heon Kim, Hyeun Wook Chang, Kyung Eun Doh, Hee Kyung Rhee, Hea Young Park Choo

Research output: Contribution to journalArticlepeer-review

20 Citations (Scopus)

Abstract

5-Lipoxygenase (5-LOX) is important enzyme in the biosynthesis of leukotrienes, and is a potential target in the treatment of asthma and allergy. We designed and synthesized a series of benzoxazoles and benzothiazoles as 5-LOX inhibitors. Fourteen compounds prepared showed the inhibition of LTC4 formation with IC50 value of 0.12-23.88 μM. Also two compounds 2d and 2g showed improved airway hypersensitiveness.

Original languageEnglish
Pages (from-to)7580-7585
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number21
DOIs
Publication statusPublished - 2010 Nov 1

Bibliographical note

Funding Information:
This work was supported by a Grant (title: Development of new technology for next generation, NBM1200513 ) from Ministry of Knowledge Economy in Korea .

All Science Journal Classification (ASJC) codes

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

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