Design and synthesis of quinazolinyl acetamides for their analgesic and anti-inflammatory activities

被引：2

作者：

Alagarsamy, Veerachamy ^{[1
]}

Solomon, Viswas Raja ^{[2
]}

Sulthana, Mohaideen Thasthagir ^{[1
]}

Vijay, Meduri Satyasai ^{[1
]}

Narendhar, Bandi ^{[1
]}

机构：

[1] MNR Coll Pharm, Med Chem Res Lab, Sangareddy 502294, Telangana, India

[2] Univ Sydney, Fac Pharm, Sydney, NSW 2006, Australia

来源：

ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES | 2015年 / 70卷 / 08期

关键词：

analgesic; anti-inflammatory; quinazoline; ulcer index; PHARMACOLOGICAL EVALUATION; AGENTS; DRUGS; AMINO-3H-QUINAZOLIN-4-ONES; DERIVATIVES;

D O I：

10.1515/znb-2015-0035

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A variety of novel 2-(substituted)-N-(4-oxo-2-phenylquinazolin-3(3H)-yl) acetamides were synthesized by the reaction of 2-chloro-N-(4-oxo-2-phenylquinazolin-3(3H)-yl) acetamide with various amines. The starting material, 2-chloro-N-(4-oxo-2-phenylquinazolin-3(3H)-yl) acetamide, was synthesized from anthranilic acid by the multistep process. The title compounds were investigated for analgesic, anti-inflammatory, and ulcerogenic index activities. Among those, the compound 2-(ethylamino)-N-(4-oxo-2-phenylquinazolin-3(3H)-yl) acetamide (V9) showed most potent analgesic and anti-inflammatory activities of the series and it is moderately more potent compared to the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential compared to aspirin.

引用

页码：597 / 604

页数：8

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