Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors
Hyunmin Song1, Sei-Ryang Oh, Hyeong-Kyu Lee
1School of pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
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 μM. Also two compounds 2d and 2g showed improved airway hypersensitiveness.
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