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Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

Authors
Song, HyunminOh, Sei-RyangLee, Hyeong-KyuHan, GyoonheeKim, Joo-HeonChang, Hyeun WookDoh, Kyung-EunRhee, Hee-KyungChoo, 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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