Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors.
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.
Song
Hyunmin
H
School of pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
Oh
Sei-Ryang
SR
Lee
Hyeong-Kyu
HK
Han
Gyoonhee
G
Kim
Joo-Heon
JH
Chang
Hyeun Wook
HW
Doh
Kyung-Eun
KE
Rhee
Hee-Kyung
HK
Choo
Hea-Young Park
HY
D000485:Allergens / Q000633:toxicity; D000818:Animals; D001094:Arachidonate 5-Lipoxygenase / Q000737:chemistry* / Q000378:metabolism; D001249:Asthma / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D051379:Mice; D013329:Structure-Activity Relationship
D000485:Allergens; D001583:Benzoxazoles; D016859:Lipoxygenase Inhibitors; D001094:Arachidonate 5-Lipoxygenase