SYNTHESIS AND NEUROKININ ANTAGONIST ACTIVITY OF 2-BENZYLIDENE- AND 2-BENZYL-3-BENZYLAMINO QUINUCLIDINES

Molecular modeling studies based on the potent NK-1 antagonist CP-96,3 45 led us to the identification of some 2-benzylidene- and 2-benzyl-3- benzylaminoquinuclidine derivatives as potential antagonists at the NK receptor subtypes. The synthesized compounds, whose Z/E isomerism has been defined by X-ray analysis, show only moderate potency on the thr ee neurokinin receptors. The possibile reasons of the lo w potency exh ibited by the tested compounds are discussed.