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作为抗炎、抗菌和抗真菌剂的二氢嘧啶酮衍生物的微波辅助合成及生物学评价

Microwave-assisted synthesis and biological evaluation of dihydropyrimidinone derivatives as anti-inflammatory, antibacterial, and antifungal agents.

作者信息

Bhatewara Anjna, Jetti Srinivasa Rao, Kadre Tanuja, Paliwal Pradeep, Jain Shubha

机构信息

Laboratory of Heterocycles, School of Studies in Chemistry and Biochemistry, Vikram University, Ujjain, Madhya Pradesh 456010, India.

出版信息

Int J Med Chem. 2013;2013:197612. doi: 10.1155/2013/197612. Epub 2013 Apr 15.

Abstract

A simple protocol for the efficient preparation of aryl and heteroaryl substituted dihydropyrimidinone has been achieved via initial Knoevenagel, subsequent addition, and final cyclization of aldehyde, ethylcyanoacetate, and guanidine nitrate in the presence of piperidine as a catalyst in solvent-free under microwave irradiation. The synthesized compounds showed a good anti-inflammatory, antibacterial, and antifungal activity.

摘要

通过在无溶剂条件下微波辐射下,以哌啶为催化剂,使醛、氰基乙酸乙酯和硝酸胍先进行克诺文纳格尔反应,随后进行加成反应,最后进行环化反应,实现了一种高效制备芳基和杂芳基取代二氢嘧啶酮的简单方法。合成的化合物表现出良好的抗炎、抗菌和抗真菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98f7/4238236/4dbf8e600297/IJMC2013-197612.sch.001.jpg

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