Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors
- Authors
- 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
- Issue Date
- 1-Nov-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Benzoxazoles; 5-LOX inhibitors; Airway hypersensitiveness
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.21, pp 7580 - 7585
- Pages
- 6
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 18
- Number
- 21
- Start Page
- 7580
- End Page
- 7585
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/13095
- DOI
- 10.1016/j.bmc.2010.08.047
- ISSN
- 0968-0896
1464-3391
- 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 mu M. Also two compounds 2d and 2g showed improved airway hypersensitiveness. (C) 2010 Elsevier Ltd. All rights reserved.
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