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一些 1,3,4-噁二唑衍生物的合成及生物评价。

Synthesis and biological evaluation of some 1,3,4-oxadiazole derivatives.

机构信息

Department of Chemistry, Mangalore University, Mangalagangothri-574 199, Karnataka, India.

出版信息

Eur J Med Chem. 2010 Nov;45(11):5225-33. doi: 10.1016/j.ejmech.2010.08.039. Epub 2010 Aug 21.

Abstract

The acid hydrazides (2) derived from ibuprofen and 4-methylthiophenyl acetic acids have been subjected to cyclization with carbon disulphide under basic conditions to yield 1,3,4-oxadiazol-2-thiones (3) which on aminomethylation with formaldehyde and secondary amines afforded a series of Mannich bases (4 and 5). Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. The newly synthesized compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities.

摘要

从布洛芬和 4-甲基噻吩乙酸衍生的酸酰肼(2)在碱性条件下与二硫化碳环化,生成 1,3,4-恶二唑-2-硫酮(3),然后用甲醛和仲胺进行氨甲基化,得到一系列曼尼希碱(4 和 5)。通过薄层色谱法确认了化合物的纯度。这些化合物的结构是基于元素分析和光谱研究确定的。新合成的化合物进行了抗炎、镇痛、致溃疡和抗菌活性评价。

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