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白三烯类(LTC_4,LTD_4和LTE_4)已证实为慢反应过敏物质的生物活性成分。由致敏的人和动物肺组织释放的这些天然物质会引起长时间的支气管收缩、微血管通透性增加及粘液分泌增多,它们与哮喘及多种速发过敏症有关,也与非免疫学的肺、心血管和肾脏的疾病有关。已报道的大多数白三烯拮抗剂与原型拮抗剂FPL 55712的结构相似,但对LTD_4受体并不显示高亲和力。本文介绍新发现的一系列〔(苯辛基/苯基〕丙酸类强效高亲和力肽白三烯受体拮抗剂,重点介绍3-〔(2-羧乙基)硫代〕-3-〔2-(8-苯辛基)苯
Leukotrienes (LTC_4, LTD_4 and LTE_4) have been shown to be bioactive components of slow-reacting allergic substances. These natural substances released by sensitized human and animal lung tissue cause prolonged bronchoconstriction, increased microvascular permeability and increased mucus secretion, which are associated with asthma and various hypersensitivity conditions, as well as with non-immunological Lung, cardiovascular and kidney disease. Most of the reported leukotriene antagonists have similar structures to the prototype antagonist FPL 55712 but do not show high affinity for the LTD 4 receptor. This article presents a series of newly discovered potent, high affinity peptide leukotriene receptor antagonists of [(phenyloctylphenyl) propionate], focusing on 3 - [(2-carboxyethyl) thio] -3- [2- (8-phenyloctyl) benzene