Molecular Pharmacology, Vol 10, 425-437, Copyright © 1974 by the American Society for Pharmacology and Experimental Therapeutics

The Conformation of Neuroleptic Drugs

¹ Laboratoire de Chimie Physique et de Cristallographie, Institut Lavoisier, Université de Louvain, Belgium

A study of the conformation of neuroleptic durgs by X-ray diffraction and simple conformational calculations has revealed some relationships among the relative arrangements of possible pharmacodynamic groups for these substances. A hydrogen bond donor at an appropriate distance from the basic nitrogen common to most neuroleptics often results in an enhancement of activity.

Note:
ACKNOWLEDGMENTS I am much indebted to Dr. P. A. J. Janssen and Dr. J. Tollenaere for stimulating discussions. I also thank Professor M. Van Meerssche for his interest in this work.

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