Dual antagonists of platelet activating factor and histamine 3. synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines

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.