Basicity, Lipophilicity, and Lack of Receptor Interaction of N??Aminoalkylbenzamides and N??Aminoalkyl??o??anisamides as Model Compounds of Dopamine Antagonists

L Anker, B Testa, H Van De Waterbeemd…

Index: Anker; Testa; Van de Waterbeemd; et al. Helvetica Chimica Acta, 1983 , vol. 66, # 2 p. 542 - 556

Full Text: HTML

Citation Number: 11

Abstract

Abstract N-Aminoalkylbenzamides and N-aminoalkyl-o-methoxybenzamides have been prepared and examined for their pK a, log P and dopamine receptor affinity. The pK a values range from ca. 7.5 for the derivatives having a one-C-atom side-chain, to ca. 10.3 for the N- aminobutyl derivatives. These variations with chain length are satisfactoryly explained by a field model. The variations in (log P)-values as a function of chain length and substitution ...