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 journalArticle

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

All Science Journal Classification (ASJC) codes

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

Fingerprint Dive into the research topics of 'Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors'. Together they form a unique fingerprint.

  • Cite this

    Song, H., Oh, S. R., Lee, H. K., Han, G., Kim, J. H., Chang, H. W., Doh, K. E., Rhee, H. K., & Choo, H. Y. P. (2010). Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors. Bioorganic and Medicinal Chemistry, 18(21), 7580-7585. https://doi.org/10.1016/j.bmc.2010.08.047