[5-Aroyl-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-carboxylic acids: synthesis and analgesic and neurobehavioral activity].
Reaction between 1-(2-aminomethylphenyl)-1H-pyrrole hydrochloride and methyl 2-methoxyglicolate in methanol afforded methyl 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-carboxylate. Aroylation at the 5-position and subsequent hydrolysis of the ester function led to 5-aroyl-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-ca rboxylic acids. The pharmacological profile of these acids has been studied with regard to analgesic, antiinflammatory and neuropsychobehavioural effects.
Massa
S
S
Dipartimento di Studi Farmaceutici-Università di Roma La Sapienza.
Corelli
F
F
Artico
M
M
Mai
A
A
Silvestri
R
R
Pantaleoni
G C
GC
Palumbo
G
G
Fanini
D
D
Giorgi
R
R
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis; D000927:Anticonvulsants / Q000138:chemical synthesis; D001522:Behavior, Animal / Q000187:drug effects*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D008297:Male; D051379:Mice; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D011758:Pyrroles; D001569:Benzodiazepines
Acidi 5-aroil-5,6-diidro-4H-pirrolo[1,2-a][1,4]benzodiazepin-4-carbossilici: sintesi ed attività analgesica e neurocomportamentale.