Australian Journal of Chemistry Australian Journal of Chemistry Society
An international journal for chemical science

Synthesis and Preliminary Pharmacological Evaluation of 4´-Arylmethyl Analogues of Clozapine. I. The Effect of Aromatic Substituents

B. Capuano, I. T. Crosby, E. J. Lloyd and D. A. Taylor

Australian Journal of Chemistry 55(9) 565 - 576
Published: 18 October 2002


As part of a research program to develop compounds with mixed dopamine D4 and serotonin 5-HT2A antagonist activity with potential for the treatment of schizophrenia, we report a family of compounds based on structural modification of the atypical antipsychotic, clozapine (2). The chemical synthesis, structural characterization and pharmacological evaluation of a series 4´-arylmethyl analogues of clozapine are described. Preliminary receptor binding data are presented, examining primarily the electronic and positional effects of substituents on the introduced arylmethyl group, and secondarily the nature of the aryl ring.

© CSIRO 2002

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