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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
- 발행일
- 2010-11-01
- 유형
- Article
- 권
- 18
- 호
- 21
- 페이지
- 7580 ~ 7585