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

doi:10.1016/j.bmc.2010.08.047

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 journal › Article › peer-review

26 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 language	English
Pages (from-to)	7580-7585
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	21
DOIs	https://doi.org/10.1016/j.bmc.2010.08.047
Publication status	Published - 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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10.1016/j.bmc.2010.08.047

Cite this

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title = "Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors",

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.",

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T1 - Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

AU - Song, Hyunmin

AU - Oh, Sei Ryang

AU - Lee, Hyeong Kyu

AU - Han, Gyoonhee

AU - Kim, Joo Heon

AU - Chang, Hyeun Wook

AU - Doh, Kyung Eun

AU - Rhee, Hee Kyung

AU - Choo, Hea Young Park

N1 - 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 .

PY - 2010/11/1

Y1 - 2010/11/1

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AB - 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.

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Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

Abstract

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