Abstract

a macrocyclic benzamide was synthesized and its affinities for 5-HT 3, 5-HT 4 and D 2 receptors were evaluated in binding assays. It was compared to reference benzamldes possessing a piperidine ring with varlous orlentations of the N-substituent. It was clearly demonstrated that the orientation of the basic nitrogen atom lone pair is an essential structural parameter in the recognition of 5-HT 3 and 5-HT 4 receptors.

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