[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole and 2-(4'-pyridinyl)-5R-benzimidazoles. Analgesic activity and effect on conditioned avoidance response].
Sixteen 2-(4'R')phenyl-5R-benzimidazoles and two 2-(4'-pyridinyl)-5R-benzimidazoles were prepared and tested, together with 2-phenylbenzimidazole, for their activity on the acquisition of a conditioned avoidance response in rats and for analgesic activity in mice, and compared with chlorpromazine and acetylsalicylic acid. Several compounds inhibit strongly the acquisition of a C.A.R., with 2-(4'-alkoxy)phenylbenzimidazoles (XVI) and (XVII) clearly exceeding chlorpromazine. Analgesic activity is also generally present in the examined compounds; those bearing in the position 5 a trifluoromethyl or an acetyl group exhibit an activity higher than that of acetylsalicylic acid. Deconditioning and analgesic activities are not correlated with each other.
Istituto di Chimica Farmaceutica e Tossicologia, Università di Sassari.
G
G
Paglietti
M A
MA
Pirisi
M
M
Loriga
G E
GE
Grella
F
F
Sparatore
M
M
Satta
P
P
Manca
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D008297:Male; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D001562:Benzimidazoles; D011725:Pyridines; C004453:bendazole
Preparazione e attivita' farmacologica di 2-(4'R')fenil-5R-benzimidazoli e 2-(4'piridinil)-5R-benzimidazoli. Attività analgesica e sull'acquisizione di una risposta condizionata di evitamento.