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一些新型3H-喹唑啉-4-酮衍生物的合成、镇痛及抗炎活性评价

Synthesis, analgesic and anti-inflammatory evaluation of some new 3H-quinazolin-4-one derivatives.

作者信息

Alafeefy Ahmed M, Kadi Adnan A, El-Azab Adel S, Abdel-Hamide Sami G, Daba Mohamad-Hesham Y

机构信息

Department of Pharmaceutical Chemistry, King Saud University, Riyadh, Saudi Arabia.

出版信息

Arch Pharm (Weinheim). 2008 Jun;341(6):377-85. doi: 10.1002/ardp.200700271.

Abstract

In this study, we have synthesized a series of 3H-quinazolin-4-ones in order to obtain new compounds with potential analgesic and anti-inflammatory activity. The structures of the newly synthesized compounds were confirmed by means of infrared, nuclear magnetic resonance and mass spectroscopy. Some compounds were evaluated for their analgesic and anti-inflammatory activities by writhing and carrageenan-induced rat paw edema tests, respectively. In comparison to the standard drug indomethacine, compounds 4, 6c, 12-14, 16, 18, 19, and 22 induced significant reduction in the writhing response while compounds 6c, 12, 14, 16, 18, and 22 produced a good dose-dependent anti-inflammatory activity. The best dual analgesic / anti-inflammatory relative activity was observed with compounds 6c, 14, 16, 18, and 22.

摘要

在本研究中,我们合成了一系列3H-喹唑啉-4-酮,以获得具有潜在镇痛和抗炎活性的新化合物。通过红外光谱、核磁共振光谱和质谱对新合成化合物的结构进行了确证。分别通过扭体试验和角叉菜胶诱导的大鼠足跖肿胀试验对一些化合物的镇痛和抗炎活性进行了评价。与标准药物吲哚美辛相比,化合物4、6c、12 - 14、16、18、19和22可显著降低扭体反应,而化合物6c、12、14、16、18和22具有良好的剂量依赖性抗炎活性。化合物6c、14、16、18和22表现出最佳的双重镇痛/抗炎相对活性。

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