110319-90-9Relevant academic research and scientific papers
2-Phenylpyrroles as Conformationally Restricted Benzamide Analogues. A New Class of Potential Antipsychotics. 1.
Wijngaarden, Ineke van,Kruse, Chris G.,Hes, Roelof van,Heyden, Jan A. M.van der,Tulp, Martin Th. M.
, p. 2099 - 2104 (1987)
2-Phenylpyrroles were synthesized as conformationally restricted analogues of the substituted benzamide sultopride and the butyrophenones haloperidol and fluanisone.Dopamine antagonistic activity is maintained if the 2-phenylpyrrole side chain is linked t
2-Phenylpyrroles as Conformationally Restricted Benzamide Analogues. A New Class of Potential Antipsychotics. 2
Wijngaarden, Ineke van,Kruse, Chris G.,Heyden, Jan A. M. van der,Tulp, Martin Th. M.
, p. 1934 - 1940 (2007/10/02)
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-methyl>pyrrole (1), the prototype of a new class of sodium-independent atypical dopamine D-2 antagonists, resulted in 2-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.
