3-(3-Ethylphenyl)-2-substituted hydrazino-3H-quinazolin-4-one Derivatives: New Class of Analgesic and Anti-Inflammatory Agents

被引:51
作者
Alagarsamy, V. [1 ]
Solomon, V. Raja [2 ]
Sheorey, R. V. [3 ]
Jayakumar, R. [1 ]
机构
[1] MNR Coll Pharm, Med Chem Res Lab, Sangareddy 502294, Andhra Pradesh, India
[2] Cent Drug Res Inst, Med Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[3] Raipur Inst Technol, Inst Pharm, Dept Pharmacol, Raipur 492101, Madhya Pradesh, India
关键词
analgesic; anti-inflammatory activity; quinazoline; structure-activity relationship; PHARMACOLOGICAL EVALUATION; ANTIBACTERIAL ACTIVITIES; 2,3-DISUBSTITUTED QUINAZOLIN-4(3H)-ONES; AMINO-3H-QUINAZOLIN-4-ONES; QUINAZOLIN-4-(3H)-ONES; QUINAZOLINES;
D O I
10.1111/j.1747-0285.2009.00794.x
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A new series of 3-(3-ethylphenyl)-2-substituted hydrazino-3H-quinazolin-4-ones were synthesized by reacting the amino group of 2-hydrazino-3-(3-ethylphenyl)-3H-quinazolin-4-one with a variety of aldehydes and ketones. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index behavior. The compound 2-(N'-3-pentylidene-hydrazino)-3-(3-ethylphenyl)-3H-quinazolin-4-one (AS2) emerged as the most active compound in exhibiting analgesic activity and the compound 2-(N'-2-pentylidene-hydrazino)-3-(3-ethylphenyl)-3H-quinazolin-4-one (AS3) emerged as the most active compound in exhibiting anti-inflammatory activity; and these compounds are moderately potent when compared with the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared with aspirin.
引用
收藏
页码:471 / 479
页数:9
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