Alagarsamy V, Meena S, Ramaseshu K V, Solomon V Raja, Kumar T Durai Ananda, Thirumurugan K
Medicinal Chemistry Research Laboratory, Dayananda Sagar College of Pharmacy, Kumaraswamy Layout, Bangalore 560 078, India.
Chem Biol Drug Des. 2007 Sep;70(3):254-60. doi: 10.1111/j.1747-0285.2007.00548.x.
A variety of novel 3-butyl-2-substituted amino-3H-quinazolin-4-ones were synthesized by reacting the amino group of 3-butyl-2-hydrazino-3H-quinazolin-4-one with various aldehydes and ketones. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. The compound 3-butyl-2-(1-methylbutylidene-hydrazino)-3H-quinazolin-4-one (AS3) emerged as the most active analgesic agent. Compound 3-butyl-2-(1-ethylpropylidene-hydrazino)-3H-quinazolin-4-one (AS2) emerged as the most active anti-inflammatory agent and is moderately more potent when compared to the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared to aspirin.
通过使3-丁基-2-肼基-3H-喹唑啉-4-酮的氨基与各种醛和酮反应,合成了多种新型的3-丁基-2-取代氨基-3H-喹唑啉-4-酮。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3-丁基-2-(1-甲基亚丁基肼基)-3H-喹唑啉-4-酮(AS3)是最具活性的镇痛剂。化合物3-丁基-2-(1-乙基亚丙基肼基)-3H-喹唑啉-4-酮(AS2)是最具活性的抗炎剂,与参考标准双氯芬酸钠相比,活性略高。有趣的是,与阿司匹林相比,测试化合物仅显示出轻微的致溃疡潜力。