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含氟4-苯并呋喃-2-基-6-苯基嘧啶-2-胺的微波辅助合成及其体外抗菌活性

Microwave assisted synthesis and in vitro antimicrobial activities of fluorine containing 4-benzofuran-2-yl-6-phenyl-pyrimidin-2-ylamines.

作者信息

Chundawat Tejpal Singh, Sharma Nutan, Bhagat Sunita

机构信息

Organic Synthesis Research Laboratory, Department of Chemistry, A.R.S.D. College, University of Delhi, New Delhi-110021, India.

出版信息

Med Chem. 2014 Jun;10(4):409-17. doi: 10.2174/15734064113099990036.

Abstract

A series of new analogs fluorine containing heterocyclic system viz. 4-benzofuran-2-yl-6-phenyl-pyrimidin-2- ylamine has been synthesized and evaluated for in vitro antibacterial and antifungal activities. Microwave assisted Claisen-Schmidt condensation of 2-acetylbenzofuran (3) with fluorinated benzaldehydes (4) afforded corresponding fluorinated chalcones (5a-g). The cyclocondensation of chalcones with guanidine hydrochloride in alkaline media under microwave resulted in the formation of corresponding fluorine containing 4-benzofuran-2-yl-6-phenyl-pyrimidin-2- ylamines (6a-g). All the synthesized compounds have been characterized on the basis of analytical and spectral data and were screened for their antibacterial and antifungal activities. Some of the synthesized compounds showed good antimicrobial activities against bacteria and fungi.

摘要

一系列新的含氟杂环系统类似物,即4-苯并呋喃-2-基-6-苯基嘧啶-2-胺已被合成,并对其体外抗菌和抗真菌活性进行了评估。2-乙酰基苯并呋喃(3)与氟化苯甲醛(4)在微波辅助下进行克莱森-施密特缩合反应,得到相应的氟化查耳酮(5a-g)。查耳酮与盐酸胍在碱性介质中于微波条件下进行环缩合反应,生成相应的含氟4-苯并呋喃-2-基-6-苯基嘧啶-2-胺(6a-g)。所有合成的化合物均通过分析和光谱数据进行了表征,并对其抗菌和抗真菌活性进行了筛选。一些合成的化合物对细菌和真菌表现出良好的抗菌活性。

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