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Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational
J J Piwinski1, J K Wong, M J Green
1Department of Chemical Research, Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
Bioorganic & Medicinal Chemistry Letters
|February 6, 1999
Abstract:
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.