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新型吲哚噻二嗪并氮杂环丁酮和吲哚噻二嗪并噻唑烷酮类化合物的合成与评价及其作为抗菌剂的应用。

Synthesis and evaluation of novel indolylthiadiazinoazetidinones and indolylthiadiazinothiazolidinones as antimicrobial agents.

机构信息

Department of Pharmacology, L. L. R. M. Medical College, Meerut, India.

出版信息

Arch Pharm (Weinheim). 2010 Feb;343(2):98-107. doi: 10.1002/ardp.200900203.

Abstract

Some new 5-methoxy/ethoxy-2,3-[2'-(3''-chloro-2''-oxo-4''-substituted-aryl-1''-azetidinyl)-1',3',4'-thiadiazino]indoles 13-20 and 5-methoxy/ethoxy-2,3-[2'-(2''-substituted-aryl-4''-oxo-1'',3''-thiazolidin-3''-yl)-1',3',4'-thiadiazino]indoles 21-28 have been synthesized from 5-methoxy/ethoxy-2,3-[2'-(substituted-benzylidinylimino)-1',3',4'-thiadiazino]indoles 5-12. These newly synthesized compounds were characterized by elemental and spectral analysis. Further, compounds 5-28 of the present series have been screened for their antibacterial and antifungal activities. Both minimal inhibitory concentration (MIC) and inhibition zones were determined in order to monitor the efficacy of the synthesized compounds. Compounds 14 and 16 were found to be the most potent members of the present series, they showed maximal antibacterial and antifungal properties much better than the standard drugs.

摘要

一些新的 5-甲氧基/乙氧基-2,3-[2'-(3''-氯-2''-氧代-4''-取代芳基-1''-氮杂环丁基)-1',3',4'-噻二唑]吲哚 13-20 和 5-甲氧基/乙氧基-2,3-[2'-(2''-取代芳基-4''-氧代-1'',3''-噻唑烷-3''-基)-1',3',4'-噻二唑]吲哚 21-28 是由 5-甲氧基/乙氧基-2,3-[2'-(取代苄亚氨基)咪唑]吲哚 5-12 合成的。这些新合成的化合物通过元素分析和光谱分析进行了表征。此外,还对本系列化合物 5-28 进行了抗菌和抗真菌活性筛选。为了监测合成化合物的功效,测定了最小抑菌浓度(MIC)和抑菌圈。发现化合物 14 和 16 是本系列中最有效的成员,它们表现出的最大抗菌和抗真菌特性明显优于标准药物。

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