M. Langlois et al., SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF A MACROCYCLIC BENZAMIDE, Bioorganic & medicinal chemistry letters, 5(8), 1995, pp. 795-798
a macrocyclic benzamide was synthesized and its affinities for 5-HT3,
5-HT4 and D-2 receptors were evaluated in binding assays. It was compa
red to reference benzamides possessing a piperidine ring with various
orientations of the N-substituent. It was clearly demonstrated that th
e orientation of the basic nitrogen atom lone pair Is an essential str
uctural parameter In the recognition of 5-HT3 and 5-HT4 receptors.