Houlihan W J, Cheon S H, Parrino V A, Handley D A, Larson D A
Sandoz Research Institute, East Hanover, New Jersey 07936.
J Med Chem. 1993 Oct 15;36(21):3098-102. doi: 10.1021/jm00073a008.
In an effort to determine the effect of modification of the imidazo[2,1-a]isoquinoline portion of the PAF-receptor antagonist SDZ 64-412 (1), several new analogs were prepared and evaluated in vitro and in vivo. One of these, 5-[4-[2-(3,4,5-trimethoxyphenyl)ethyl]phenyl]-2,3-dihydroimidazo [1,2-a]thieno[2,3-c]pyridine (6) was 4-5 times more potent than 1 in inhibiting PAF-induced bronchoconstriction and hemoconcentration when administered po to the guinea pig.
为了确定对血小板活化因子（PAF）受体拮抗剂SDZ 64 - 412（1）的咪唑并[2,1 - a]异喹啉部分进行修饰的效果，制备了几种新的类似物，并在体外和体内进行了评估。其中之一，5 - [4 - [2 - (3,4,5 - 三甲氧基苯基)乙基]苯基] - 2,3 - 二氢咪唑并[1,2 - a]噻吩并[2,3 - c]吡啶（6），经口服给予豚鼠时，在抑制PAF诱导的支气管收缩和血液浓缩方面比1强4 - 5倍。
