Hori M, Iemura R, Hara H, Sukamoto T, Ito K, Ohtaka H
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1991 Feb;39(2):367-71. doi: 10.1248/cpb.39.367.
A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity than such reference compounds as aniracetam, idebenone and bifemelane at a wide dose range (1-30 mg/kg]. Compound 4 also exhibited potent anticonvulsive and antihypoxic activities, and was selected as the most promising nootropic candidate agent.
合成了一系列4-烷氧基-2-(1-哌嗪基)喹唑啉衍生物,并在单次被动回避任务中评估了它们逆转东莨菪碱诱导的学习障碍的能力(抗遗忘活性)。2-(4-烯丙基-1-哌嗪基)-4-戊氧基喹唑啉(4)在较宽剂量范围(1-30mg/kg)内显示出比阿尼西坦、艾地苯醌和比芬美兰等参考化合物更强的抗遗忘活性。化合物4还表现出强效的抗惊厥和抗缺氧活性,并被选为最有前景的促智候选药物。