Synthesis, analgesic and anti-inflammatory activities of novel 3-(4-acetamido-benzyl)-5-substituted-1,2,4-oxadiazoles

Synthesis, analgesic and anti-inflammatory activities of novel 3-(4-acetamido-benzyl)-5-substituted-1,2,4-oxadiazoles
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DOI:
10.1016/j.ejmech.2008.05.022
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发表时间:
2009-02-01
影响因子:
6.7
通讯作者:
Patil, C. R.
Patil, C. R.
中科院分区:
医学1区
文献类型:
--
作者:
Farooqui, Mazahar;Bora, Rajesh;Patil, C. R.

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合成了一系列3-(4-乙酰氨基苄基)-5-取代-1,2,4-恶二唑(7a-7 n),并分别采用小鼠醋酸扭体法和角叉菜胶致小鼠足肿胀法进行镇痛和抗炎活性的筛选。化合物7 i和7 m的镇痛活性为上级,而化合物7 d、7 c、7 f和7 j的镇痛活性与对照品双氯芬酸钠相当。发现化合物6、7 c、7 e、7 f、7 i、7 l、7 m和7 n的抗炎活性比用作对照的双氯芬酸钠的抗炎活性好上级,而发现化合物7 d和7 g与对照化合物等效。(c)2008年,Elsevier Masson SAS。All rights reserved.
A series of 3-(4-acetamido-benzyl)-5-substituted-1,2,4-oxadiazoles (7a-7n) were synthesized and screened for analgesic and in vivo anti-inflammatory activities using acetic acid writhing in mice model and carrageenan-induced paw oedema method in mice, respectively. The analgesic activity of compounds 7i and 7m is superior while that of 7d, 7c, 7f and 7j is equal to the reference standard, diclofenac sodium. The anti-inflammatory activity of compounds 6, 7c, 7e, 7f, 7i, 7l, 7m and 7n is found to be superior than that of diclofenac sodium which is used as a reference, while compounds 7d and 7g are found to be equipotent with the reference compound. (c) 2008 Elsevier Masson SAS. All rights reserved.