Sato M, Arimoto M, Ueno K, Kojima H, Yamasaki T, Sakurai T, Kasahara A
J Med Chem. 1978 Nov;21(11):1116-20. doi: 10.1021/jm00209a005.
A series of 1-(4-fluorophenyl)-4-(1-piperidinyl)-1-butanones substituted with benzimidazole, benzotriazole, or quinoxaline at the 4 position of the piperidine ring was synthesized and subjected to neuroleptic tests. Neuroleptic activities of several compounds were comparable to those of haloperidol. In particular, 4-[4-(2,3-dihydro-2-thioxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone (10) was characterized by having a potent neuroleptic activity with less liability to the extrapyramidal side effect.
合成了一系列在哌啶环4位被苯并咪唑、苯并三唑或喹喔啉取代的1-(4-氟苯基)-4-(1-哌啶基)-1-丁酮，并进行了抗精神病测试。几种化合物的抗精神病活性与氟哌啶醇相当。特别是，4-[4-(2,3-二氢-2-硫代-1H-苯并咪唑-1-基)-1-哌啶基]-1-(4-氟苯基)-1-丁酮（10）的特点是具有强大的抗精神病活性，且锥体外系副作用较小。
