title: Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors.
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.
authors.affiliation: School of pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors.forename: Hyunmin
authors.initials: H
authors.lastname: Song
authors.forename: Sei-Ryang
authors.initials: SR
authors.lastname: Oh
authors.forename: Hyeong-Kyu
authors.initials: HK
authors.lastname: Lee
authors.forename: Gyoonhee
authors.initials: G
authors.lastname: Han
authors.forename: Joo-Heon
authors.initials: JH
authors.lastname: Kim
authors.forename: Hyeun Wook
authors.initials: HW
authors.lastname: Chang
authors.forename: Kyung-Eun
authors.initials: KE
authors.lastname: Doh
authors.forename: Hee-Kyung
authors.initials: HK
authors.lastname: Rhee
authors.forename: Hea-Young Park
authors.initials: HY
authors.lastname: Choo
mesh_terms: 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
chemical_list: D000485:Allergens; D001583:Benzoxazoles; D016859:Lipoxygenase Inhibitors; D001094:Arachidonate 5-Lipoxygenase