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

18 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

Fingerprint

Benzothiazoles
Benzoxazoles
Allergies
Arachidonate 5-Lipoxygenase
Lipoxygenase Inhibitors
Leukotriene C4
Leukotrienes
Biosynthesis
Inhibitory Concentration 50
Hypersensitivity
Asthma
Derivatives
Enzymes

All Science Journal Classification (ASJC) codes

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

Cite this

Song, Hyunmin ; Oh, Sei Ryang ; Lee, Hyeong Kyu ; Han, Gyoonhee ; Kim, Joo Heon ; Chang, Hyeun Wook ; Doh, Kyung Eun ; Rhee, Hee Kyung ; Choo, Hea Young Park. / Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors. In: Bioorganic and Medicinal Chemistry. 2010 ; Vol. 18, No. 21. pp. 7580-7585.
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Song, H, Oh, SR, Lee, HK, Han, G, Kim, JH, Chang, HW, Doh, KE, Rhee, HK & Choo, HYP 2010, 'Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors', Bioorganic and Medicinal Chemistry, vol. 18, no. 21, pp. 7580-7585. https://doi.org/10.1016/j.bmc.2010.08.047

Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors. / Song, Hyunmin; Oh, Sei Ryang; Lee, Hyeong Kyu; Han, Gyoonhee; Kim, Joo Heon; Chang, Hyeun Wook; Doh, Kyung Eun; Rhee, Hee Kyung; Choo, Hea Young Park.

In: Bioorganic and Medicinal Chemistry, Vol. 18, No. 21, 01.11.2010, p. 7580-7585.

Research output: Contribution to journalArticle

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