Structural analysis of 5-HT 3 receptor antagonists: synthesis and pharmacological activity of various aromatic esters or amides derived from tropane and 1, 2, 6- …

…, B Bremont, C Florac, V Rampillon, A Giudice

Index: Langlois; Soulier; Yang; Bremont; Florac; Rampillon; Giudice European Journal of Medicinal Chemistry, 1993 , vol. 28, # 11 p. 869 - 880

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Citation Number: 20

Abstract

Abstract Preliminary results of a structure-activity relationship in the field of 5-HT 3 receptor antagonists on the influence of the aromatic ring and steric hindrance around the basic nitrogen atom are reported. The favorable role of the naphthalene moiety substituted by a carbonyl function in position 1 was demonstrated by measuring the biological activity using the inhibition of the specific binding of [3 H] BRL 43694 and the inhibition of the Bezold- ...