Synthesis of new N-substituted benzodiazepine derivatives with potential anxiolytic activity.
In continuation of the development of antipsychotic and anxiolytic agents with a reduced propensity toward extrapyramidal side-effects, a series of N-aminoalkyl derivatives of (s)-(+)-2,3-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-(10H, 11aH)-dione was prepared. Evaluation of these compounds in revealed a very low affinity for 5-HT1A receptor.
Kossakowski
J
J
Department of Medical Chemistry, Medical University of Warsaw, Poland.
Zawadowski
T
T
Turło
J
J
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000378:metabolism; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000378:metabolism; D001933:Brain Stem / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism; D013055:Spectrophotometry, Infrared
D014151:Anti-Anxiety Agents; D011963:Receptors, GABA-A; D001569:Benzodiazepines