Paneersalvam P, Raj T, Ishar M P S, Singh B, Sharma V, Rather B A
Department of Pharmaceutical Chemistry, C. L. Baid Mehta College of Pharmacy, Jyothi Nagar, Rajiv Gandhi Salai, Thorapakkam, Chennai - 600 097, India.
Indian J Pharm Sci. 2010 May;72(3):375-8. doi: 10.4103/0250-474X.70488.
Schiff bases (9a-l) of 3-amino-6,8-dibromo-2-phenyl-quinazolin-4-(3H)-ones (8) with various substituted aldehydes were obtained by refluxing 1:1 molar equivalents of the reactants in dry ethanol for 6 h. The aminoquinazoline (8) was inturn obtained from 3,5-dibromoantharlinic acid via intermediate (7). All the synthesized compounds (9a-l) were evaluated for their anticonvulsant activity on albino mice by maximal electroshock method using phenytoin as a standard. The compound (9l) bearing a cinnamyl function displays a very high activity (82.74 %) at dose level of 100 mg/kg b.w.
3-氨基-6,8-二溴-2-苯基喹唑啉-4-(3H)-酮(8)与各种取代醛的席夫碱(9a-l)是通过将1:1摩尔当量的反应物在无水乙醇中回流6小时得到的。氨基喹唑啉(8)依次由3,5-二溴蒽醌酸通过中间体(7)制得。所有合成的化合物(9a-l)均以苯妥英为标准,采用最大电休克法对白化小鼠进行抗惊厥活性评估。具有肉桂基官能团的化合物(9l)在100 mg/kg体重的剂量水平下表现出非常高的活性(82.74%)。