Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors

Title
Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors
Author(s)
장현욱Hyunmin Son[Hyunmin Son]Sei-Ryang Oh[Sei-Ryang Oh]Hyeong-Kyu Lee[Hyeong-Kyu Lee]Gyoonhee Han[Gyoonhee Han]Joo-Heon Kim[Joo-Heon Kim]Kyung-Eun Doh[Kyung-Eun Doh]Hee-Kyung Rhee[Hee-Kyung Rhee]Hae-Young Park Choo[Hae-Young Park Choo]
Keywords
FACILE SYNTHESIS; MAST-CELLS; ASTHMA; THERAPY; DISEASES; ALLERGY; MICE
Issue Date
201011
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.21, pp.7580 - 7585
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 IC(50) 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.
URI
http://hdl.handle.net/YU.REPOSITORY/23390http://dx.doi.org/10.1016/j.bmc.2010.08.047
ISSN
0968-0896
Appears in Collections:
약학대학 > 약학부 > Articles
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