Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi 110062, India.
Arch Pharm Res. 2013 Jan;36(1):61-8. doi: 10.1007/s12272-013-0004-y.
A series of 3-[(4-substituted-benzylidene)-amino]-2-phenyl-3H-quinazolin-4-ones (5a-k) were synthesized by reacting 3-amino-2-phenyl-1H-quinazolin-4-one with p-hydroxybenzaldehyde, and then further with various alkyl/benzyl halides or substituted phenacyl bromides. The structures of the compounds were confirmed on the basis of IR, NMR, MS and elemental analysis. Anticonvulsant activities were evaluated using the MES and scPTZ tests. Some of the selected compounds were evaluated for antidepressant activity by forced swim pool test. Compound 3-[(4-butoxy-benzylidene)-amino]-2-phenyl-3H-quinazolin-4-one was emerged as the most promising anticonvulsant agent without any motor impairment effect. The whole brain GABA estimation of brain homogenate indicated that the anticonvulsant activity of above mentioned quinazolinone derivatives might be due to an increased GABA concentration.
通过将 3-氨基-2-苯基-1H-喹唑啉-4-酮与对羟基苯甲醛反应，然后进一步与各种烷基/苄基卤化物或取代的苯乙酮溴化物反应，合成了一系列 3-[(4-取代苄叉基)-氨基]-2-苯基-3H-喹唑啉-4-酮（5a-k）。基于 IR、NMR、MS 和元素分析确定了化合物的结构。使用 MES 和 scPTZ 测试评估了抗惊厥活性。通过强迫游泳池试验评估了一些选定的化合物的抗抑郁活性。3-[(4-丁氧基-苄叉基)-氨基]-2-苯基-3H-喹唑啉-4-酮作为最有前途的抗惊厥剂脱颖而出，没有任何运动障碍作用。全脑 GABA 测定表明，上述喹唑啉酮衍生物的抗惊厥活性可能是由于 GABA 浓度的增加。
