Fukushi H, Mabuchi H, Itoh K, Terashita Z, Nishikawa K, Sugihara H
Pharmaceutical Research Laboratories, I, Takeda Chemical Industries, Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1994 Mar;42(3):541-50. doi: 10.1248/cpb.42.541.
During the screening of novel platelet-activating factor (PAF) antagonists, we found that 1-(6-methoxy-3,4-dihydro-2-naphthoyl)-4- (3,4,5-trimethoxybenzyl)piperazine and its 4-(3,4,5- trimethoxybenzoyl)piperazine derivatives (1b, 2b) exerted in vitro and in vivo PAF-antagonistic activities. Modifications of the 1-acyl group, the substituent at the 4-position and the piperazine ring of 1a and 2b were examined and from this series 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclohepten-8-ylcarbonyl++ +)-4- (3,4,5-trimethoxybenzoyl)piperazine (2g) was found to be one of the most potent PAF antagonists.
在新型血小板活化因子（PAF）拮抗剂的筛选过程中，我们发现1-(6-甲氧基-3,4-二氢-2-萘甲酰基)-4-(3,4,5-三甲氧基苄基)哌嗪及其4-(3,4,5-三甲氧基苯甲酰基)哌嗪衍生物（1b、2b）具有体外和体内PAF拮抗活性。我们研究了1a和2b的1-酰基、4-位取代基以及哌嗪环的修饰情况，从该系列化合物中发现1-(2,3-二甲氧基-6,7-二氢-5H-苯并环庚烯-8-基羰基)-4-(3,4,5-三甲氧基苯甲酰基)哌嗪（2g）是最有效的PAF拮抗剂之一。
