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微波辅助合成具有脂肪酶抑制活性的新型苯并咪唑衍生物。

Microwave-assisted synthesis of new benzimidazole derivatives with lipase inhibition activity.

机构信息

Department of Chemistry, Faculty of Arts and Sciences, Recep Tayyip Erdogan University , Rize , Turkey .

出版信息

J Enzyme Inhib Med Chem. 2014 Feb;29(1):64-8. doi: 10.3109/14756366.2012.753880. Epub 2013 Jan 18.

Abstract

A practical protocol has been used for the synthesis of benzimidazoles. The reaction of iminoester hydrochlorides of phenylacetic with 4,5-dichloro-1,2-phenylenediamine under microwave irradiation leads to the benzimidazole derivatives with good yields and in short reaction times. After the synthesis of benzimidazoles, we synthesized ester and hydrazide derivatives under microwave irradiation with good yields. All compounds were evaluated with regard to pancreatic lipase activity and 3b, 3c, 5a and 6a showed lipase inhibition at various concentrations.

摘要

已使用一种实用的方案合成苯并咪唑。在微波辐射下,苯乙酸亚氨基盐酸盐与 4,5-二氯-1,2-苯二胺反应,以短反应时间和良好的收率得到苯并咪唑衍生物。合成苯并咪唑后,我们在微波辐射下合成了酯和酰肼衍生物,产率良好。所有化合物均进行了胰腺脂肪酶活性评估,在不同浓度下,3b、3c、5a 和 6a 均表现出脂肪酶抑制活性。

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