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

doi:10.1016/j.bmc.2010.08.047

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Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

Song, Hyunmin;
Oh, Sei-Ryang;
Lee, Hyeong-Kyu;
Han, Gyoonhee;
Kim, Joo-Heon;
외 4명

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37

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38

초록

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 mu M. Also two compounds 2d and 2g showed improved airway hypersensitiveness. (C) 2010 Elsevier Ltd. All rights reserved.

키워드

Benzoxazoles; 5-LOX inhibitors; Airway hypersensitiveness; FACILE SYNTHESIS; MAST-CELLS; ASTHMA; THERAPY; DISEASES; ALLERGY; MICE

제목: Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

저자: 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

DOI: 10.1016/j.bmc.2010.08.047

발행일: 2010-11-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry

권: 18

호: 21

페이지: 7580 ~ 7585

언어: ENG

출판사: PERGAMON-ELSEVIER SCIENCE LTD

발행국가: 영국

분량: 6 페이지

ISSN: E 1464-3391
P 0968-0896