Synthesis and biological activity of picobenzide (3,5-dimethyl-N-(pyridin-4-ylmethyl)benzamide) analogues as potential antipsychotic agents.
A series of analogues related to picobenzide (CAS 51832-87-2) have been prepared and have been used as starting material to obtain new trisubstituted oxazole derivatives. Two compounds showed a promising pharmacological profile in screening tests of antipsychotic activity, since they affected apomorphine-induced hyperactivity without significant effects on stereotypies.
Gradillas
Ana
A
Departamento de Químicas, Facultad de Farmacia, Universidad San Pablo CEU, Boadilla del Monte, Madrid Spain.
López
Berta
B
Braña
Miguel F
MF
Sancho
Isabel
I
Pérez-García
Carmen
C
Alguacil
Luis F
LF
D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001058:Apomorphine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D018491:Dopamine Agonists / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D006948:Hyperkinesis / Q000139:chemically induced / Q000517:prevention & control; D007202:Indicators and Reagents; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013239:Stereotyped Behavior / Q000187:drug effects; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D001549:Benzamides; D018491:Dopamine Agonists; D007202:Indicators and Reagents; C016938:picobenzide; D001058:Apomorphine