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基于β-芳酰基丙酸的1,3,4-恶二唑的合成与生物学评价

Synthesis and Biological Evaluation of beta-Aroylpropionic acid based 1,3,4-Oxadiazoles.

作者信息

Husain A, Ahuja Priyanka

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110 062, India.

出版信息

Indian J Pharm Sci. 2009 Jan;71(1):62-6. doi: 10.4103/0250-474X.51963.

Abstract

In the present investigation, two new series, 1-(4-benzylphenyl)-3-(5-substituted-1,3,4-oxadiazol-2-yl)-1-propanone and 1-(4-ethylphenyl)-3-(5-substituted-1,3,4-oxadiazol-2-yl)-1-propanone from beta-(4-benzylbenzoyl)propionic acid and beta-(4-ethylbenzoyl)propionic acid, respectively, were synthesized and tested for antiinflammatory, analgesic, lipid peroxidation, ulcerogenic and antibacterial actions. A fair number of compounds were found to have good antiinflammatory activity in carrageenan-induced rat paw edema test, while a few compounds showed significant antibacterial activity. The newly synthesized compounds showed very low ulcerogenic action.

摘要

在本研究中,分别由β-(4-苄基苯甲酰基)丙酸和β-(4-乙基苯甲酰基)丙酸合成了两个新系列的化合物,即1-(4-苄基苯基)-3-(5-取代-1,3,4-恶二唑-2-基)-1-丙酮和1-(4-乙基苯基)-3-(5-取代-1,3,4-恶二唑-2-基)-1-丙酮,并对其抗炎、镇痛、脂质过氧化、致溃疡和抗菌作用进行了测试。发现相当数量的化合物在角叉菜胶诱导的大鼠足跖肿胀试验中具有良好的抗炎活性,而少数化合物表现出显著的抗菌活性。新合成的化合物显示出极低的致溃疡作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/586f/2810053/cfdd0f8d8fdf/IJPhS-71-62-g001.jpg

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