Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

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Title
Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors
Author(s)
H Song; Sei Ryang Oh; Hyeong Kyu Lee; G Han; J H Kim; H W Chang; K E Doh; H K Rhee; H Y Park Choo
Bibliographic Citation
Bioorganic & Medicinal Chemistry, vol. 18, no. 21, pp. 7580-7585
Publication Year
2010
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.
Keyword
5-LOX inhibitorsAirway hypersensitivenessBenzoxazoles
ISSN
0968-0896
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmc.2010.08.047
Type
Article
Appears in Collections:
Ochang Branch Institute > 1. Journal Articles
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