非甾体抗炎药作为5-脂氧合酶抑制剂设计的骨架。
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
作者信息
Kolasa T, Brooks C D, Rodriques K E, Summers J B, Dellaria J F, Hulkower K I, Bouska J, Bell R L, Carter G W
机构信息
Abbott Laboratories, Abbott Park, Illinois 60064, USA.
出版信息
J Med Chem. 1997 Feb 28;40(5):819-24. doi: 10.1021/jm9606150.
PMID:9057869
Abstract
Representative nonsteroidal anti-inflammatory drug (NSAID) cyclooxygenase inhibitors such as ibuprofen, naproxen, and indomethacin were used as orally bioavailable scaffolds to design selective 5-lipoxygenase (5-LO) inhibitors. Replacement of the NSAID carboxylic acid group with a N-hydroxyurea group provided congeners with selective 5-LO inhibitory activity.
摘要
代表性的非甾体抗炎药（NSAID）环氧化酶抑制剂，如布洛芬、萘普生和吲哚美辛，被用作口服生物可利用的骨架来设计选择性5-脂氧合酶（5-LO）抑制剂。用N-羟基脲基团取代NSAID的羧酸基团，得到了具有选择性5-LO抑制活性的类似物。
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