Paglietti G, Pirisi M A, Loriga M, Grella G E, Sparatore F, Satta M, Manca P
Istituto di Chimica Farmaceutica e Tossicologia, Università di Sassari.
Farmaco Sci. 1988 Mar;43(3):215-26.
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.
制备并测试了16种2-(4'R')苯基-5R-苯并咪唑和2种2-(4'-吡啶基)-5R-苯并咪唑，连同2-苯基苯并咪唑一起，检测它们对大鼠条件性回避反应习得的活性以及对小鼠的镇痛活性，并与氯丙嗪和乙酰水杨酸进行比较。几种化合物强烈抑制条件性回避反应的习得，其中2-(4'-烷氧基)苯基苯并咪唑（XVI）和（XVII）明显超过氯丙嗪。在所检测的化合物中通常也存在镇痛活性；5位带有三氟甲基或乙酰基的那些化合物表现出高于乙酰水杨酸的活性。去条件化活性和镇痛活性彼此不相关。
