Anagnostopulos C, Bartmann W, Beck G, Below P, Bergmann A, Linz W, Schacht U, Schölkens B A, Wess G
Hoechst AG, Frankfurt (Main), FRG.
Biomed Biochim Acta. 1988;47(10-11):S190-3.
Two series of structural analogues of leukotrienes C4, D4 and E4 (LTC4, LTD4, LTE4) were prepared. The compounds were evaluated for their ability to antagonize leukotriene-induced contractions of guinea pig lung strips. In comparison to FPL-55712, compounds 1a and 2h were more potent antagonists against LTC4 (2- and 3fold, respectively) and LTD4 (6- and 60fold respectively). Moreover, in vivo compounds 1a and 2h exhibited antagonism against leukotrienes (C4, D4, E4) and PAF, the most potent mediators in bronchial asthma. 2h also showed antagonistic activity when tested by inhalation.
制备了白三烯C4、D4和E4（LTC4、LTD4、LTE4）的两个系列结构类似物。评估了这些化合物拮抗白三烯诱导的豚鼠肺条收缩的能力。与FPL-55712相比，化合物1a和2h对LTC4（分别为2倍和3倍）和LTD4（分别为6倍和60倍）是更强效的拮抗剂。此外，在体内，化合物1a和2h对白三烯（C4、D4、E4）和PAF（支气管哮喘中最有效的介质）表现出拮抗作用。通过吸入测试时，2h也显示出拮抗活性。
