Synthesis of N-(1-ethyl-4-methylhexahydro-1, 4-diazepin-6-yl) nicotinamides and their affinities for 5-HT 3 and dopamine D 2 receptors

Y Hirokawa, N Yoshida, S Kato

Index: Hirokawa, Yoshimi; Yoshida, Naoyuki; Kato, Shiro Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 12 p. 1551 - 1554

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Citation Number: 13

Abstract

A series of N-(1-ethyl-4-methylhexahydro-1, 4-diazepin-6-yl) nicotinamide derivatives were prepared and evaluated for their binding to 5-HT3 and dopamine D2 receptors. Among them, the 5-bromo-2-methoxy-6-methylaminonicotinamide 16 and its (R)-isomer were found to have potent affinities for both receptors. The affinities of (R)-16 for 5-HT3 and dopamine D2 receptors are approximately 3-fold higher than those of the corresponding benzamide ...