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简便的一锅法微波诱导无溶剂合成及螺[1,5]-苯并硫氮杂䓬-2,3'[3'H]吲哚-2[1'H]-酮的抗真菌、抗结核活性筛选

Facile one pot microwave induced solvent-free synthesis and antifungal, antitubercular screening of spiro [1,5]-benzothiazepin-2,3'[3'H]indol-2[1'H]-ones.

作者信息

Dandia Anshu, Sati Meha, Arya Kapil, Sharma Rekha, Loupy André

机构信息

Department of Chemistry, University of Rajasthan, Jaipur, India.

出版信息

Chem Pharm Bull (Tokyo). 2003 Oct;51(10):1137-41. doi: 10.1248/cpb.51.1137.

Abstract

Microwave activation coupled with dry media technique as a green chemistry procedure has been applied to synthesis of a series of some new title compounds. They have been obtained by the reaction of in situ synthesized 1,3-dihydro-3-[2-(phenyl/4-fluorophenyl)-2-oxoethylidene)-indol-2(1H)-one (4a, b) with substituted aminobenzenethiols (5a-d). The key intermediates 4a, b were also prepared in one step by this improved technique by reacting isatin and substituted acetophenones (2a, b). The results obtained under microwave irradiation when compared with that following conventional method demonstrate the versatility of the process. The title compounds 7a-e have also been screened for their antifungal and antitubercular activity, 7a and 7e showing maximum inhibition of growth of Alternaria alternata and Fusarium oxysporium and 7b, c, e revealing significant antitubercular activity.

摘要

微波活化结合干介质技术作为一种绿色化学方法已被应用于一系列新型目标化合物的合成。它们是通过原位合成的1,3-二氢-3-[2-(苯基/4-氟苯基)-2-氧代亚乙基]-吲哚-2(1H)-酮(4a, b)与取代氨基苯硫酚(5a-d)反应得到的。关键中间体4a, b也通过该改进技术由异吲哚酮和取代苯乙酮(2a, b)一步反应制备而成。与传统方法相比,微波辐射下得到的结果证明了该方法的多功能性。还对目标化合物7a-e进行了抗真菌和抗结核活性筛选,7a和7e对链格孢菌和尖孢镰刀菌的生长具有最大抑制作用,7b、c、e显示出显著的抗结核活性。

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