Alagarsamy Veerachamy, Dhanabal Kumarasamy, Parthiban Periyasamy, Anjana Gobi, Deepa Govinhan, Murugesan Balakrishnan, Rajkumar Subramanian, Beevi Abdulrahim Janath
Medicinal Chemistry Research Laboratory, Dayananda Sagar College of Pharmacy, Kumarswamy Layout, Bangalore-560 078, India.
J Pharm Pharmacol. 2007 May;59(5):669-77. doi: 10.1211/jpp.59.5.0007.
A variety of novel 3-(3-methylphenyl)-2-substituted amino-3H-quinazolin-4-ones were synthesized by reacting the amino group of 2-hydrazino-3-(3-methylphenyl)-3H-quinazolin-4-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(3-methylphenyl)-3H-quinazolin-4-one was synthesized from 3-methyl aniline. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. Compound 2-(1-ethylpropylidene-hydrazino)-3-(3-methylphenyl)-3H-quinazolin-4-one (AS2) was the most active analgesic agent. Compound 2-(1-methylbutylidene-hydrazino)-3-(3-methylphenyl)-3H-quinazolin-4-one (AS3) was the most active anti-inflammatory agent and was moderately more potent than the reference standard diclofenac sodium. The test compounds showed only mild ulcerogenic potential compared with aspirin.
通过使2-肼基-3-(3-甲基苯基)-3H-喹唑啉-4-酮的氨基与多种醛和酮反应，合成了多种新型的3-(3-甲基苯基)-2-取代氨基-3H-喹唑啉-4-酮。起始原料2-肼基-3-(3-甲基苯基)-3H-喹唑啉-4-酮由3-甲基苯胺合成。对标题化合物进行了镇痛、抗炎和致溃疡指数活性研究。化合物2-(1-乙基亚丙基肼基)-3-(3-甲基苯基)-3H-喹唑啉-4-酮(AS2)是活性最强的镇痛剂。化合物2-(1-甲基丁基亚丙基肼基)-3-(3-甲基苯基)-3H-喹唑啉-4-酮(AS3)是活性最强的抗炎剂，其效力比参考标准双氯芬酸钠略强。与阿司匹林相比，测试化合物仅显示出轻微的致溃疡潜力。
