Piwinski J J, Wong J K, Green M J, Kaminski J J, Colizzo F, Albanese M M, Ganguly A K, Billah M M, Anthes J C, West R E
Department of Chemical Research, Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
Bioorg Med Chem Lett. 1998 Dec 15;8(24):3469-74. doi: 10.1016/s0960-894x(98)00626-x.
A series of N-acyl-4-(5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin- 11-ylidene)piperazines is described that are dual antagonists of PAF and histamine. The structural requirements for activity in this series parallel those of their previously reported piperidinylidene counterparts. Whereas their global minimum energy conformations are different for both series of compounds, computer assisted molecular modeling suggests that a common bioactive conformation is possible.
描述了一系列N-酰基-4-(5,6-二氢-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基)哌嗪，它们是血小板活化因子(PAF)和组胺的双重拮抗剂。该系列化合物的活性结构要求与其先前报道的哌啶亚基类似物的结构要求相似。尽管这两个系列化合物的全局最低能量构象不同，但计算机辅助分子建模表明可能存在共同的生物活性构象。
