Journal of Medicinal Chemistry p. 1934 - 1940 (1988)
Update date:2022-07-29
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Wijngaarden, Ineke van
Kruse, Chris G.
Heyden, Jan A. M. van der
Tulp, Martin Th. M.
A series of 2-phenylpyrrole Mannich bases was synthesized and screened in pharmacological models for antipsychotic activity and extrapyramidal effects.Structure modifications of 5-(4-fluorophenyl)-2-<<4-(2-methoxyphenyl)-1-piperazinyl>methyl>pyrrole (1), the prototype of a new class of sodium-independent atypical dopamine D-2 antagonists, resulted in 2-<<4-(7-benzofuranyl)-1-piperazinyl>methyl>-5-(4-fluorophenyl)pyrrole (15), which was an even more potent and selective D-2 antagonist than the parent compound.The excellent oral activity in the apomorphine-induced climbing behavior and the conditioned avoidance response tests and the absence of catalepsy make this compound particularly promising as a potential antipsychotic with a low propensity to induce acute extrapyramidal side effects.
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