Synthesis and analgesic, anti-inflammatory activities of 3-(3-methoxyphenyl)-2-substituted amino-quinazolin-4(3H)-ones

被引：0
作者：
V. Alagarsamy
M. Gopinath
P. Parthiban
B. Subba Rao
K. Murali
V. Raja Solomon
机构：
[1] MNR College of Pharmacy,Medicinal Chemistry Research Laboratory
[2] Ratnam Institute of Pharmacy,Department of Pharmaceutical Chemistry
[3] C.L. Baid Metha College of Pharmacy,Department of Pharmaceutical Chemistry
[4] Central Drug Research Institute,Medicinal and Process Chemistry Division
来源：
Medicinal Chemistry Research | 2011年 / 20卷
关键词：
Quinazoline; Analgesic; Anti-inflammatory; Ulcer index;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A variety of novel 3-(3-methoxyphenyl)-2-substituted amino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 2-hydrazino-3-(3-methoxyphenyl)-quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(3-methoxyphenyl)-quinazolin-4(3H)-one was synthesized from 3-methoxy aniline. The title compounds were investigated for analgesic, anti-inflammatory, and ulcerogenic behavior. Among these the compound 2-(1-methyl butylidene-hydrazino)-3-(3-methoxyphenyl)-3H-quinazolin-4-one (AS3) emerged as the most active compound for the analgesic activity, while the compound 2-(1-ethyl propylidene-hydrazino)-3-(3-methyoxyphenyl)-3H-quinazolin-4-one (AS2) showed most potent anti-inflammatory activity of the series and these compounds are moderately more potent when compared to the reference standard diclofenac sodium. Interestingly the test compounds showed only mild ulcerogenic potential when compared to acetylsalicylic acid.
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页码：946 / 954
页数：8
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共 71 条
[11]  
Amuthalakshmi S(1973)Effect of bilateral adrenalectomy on production of restraint ulcers in the stomach of albino rats Can J Physiol Pharmacol 51 748-750
[12]  
Revathi R(1985)The effect of biological variables on the anti-ulcerogenic effect of vegetable plantain banana Planta Med 29 85-88
[13]  
Alagarsamy V(1980)Heat and other physiological stress-induced analgesia: catecholamine mediated and naloxone reversible response Life Sci 27 185-188
[14]  
Murugananthan G(1995)Synthesis and pharmacological evaluation of thieno[2, 3-d]pyrimidin-2, 4-dione and 5H-pyrimido [5, 4-b]indol-2, 4-dione derivatives Il Farmaco 50 689-695
[15]  
Venkateshperumal R(1945)A simple method for the uniform production of gastric ulceration in the rats Gastroenterology 5 43-61
[16]  
Alagarsamy V(1971)Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs Nat New Biol 231 232-235
[17]  
Muthukumar V(1995)New insights into the mode of action of anti-inflammatory drugs Inflamm Res 44 1-10
[18]  
Pavalarani N(2000)COX-2 selectivity and inflammatory processes Curr Med Chem 7 1145-1161
[19]  
Vasanthanathan P(1962)Carregeenin induced oedema in hind paw of the rat as assay for antiinflammatory drugs Exp Biol Med 111 544-547
[20]  
Revathi R(undefined)undefined undefined undefined undefined-undefined
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