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2-巯基苯并咪唑杂环化为含与苯并咪唑相连的-CONH-桥的β-内酰胺片段衍生物的绿色路线:对多种微生物进行体外抗菌活性筛选。

Green route for the heterocyclization of 2-mercaptobenzimidazole into beta-lactum segment derivatives containing -CONH- bridge with benzimidazole: Screening in vitro antimicrobial activity with various microorganisms.

作者信息

Desai Krunal G, Desai Kishor R

机构信息

Department of Chemistry, Faculty of Science, Synthetic Organic Chemistry Research Laboratory, Veer Narmad South Gujarat University, Udhna-Magdalla Road, Surat (west)-395 007, Gujarat State, India.

出版信息

Bioorg Med Chem. 2006 Dec 15;14(24):8271-9. doi: 10.1016/j.bmc.2006.09.017. Epub 2006 Oct 10.

Abstract

The efficient and rapid synthesis of novel azetidin-2-ones 4a-j has been established. Thus, both microwave and conventional condensation 2-{(1H-benzimidazol)-ylthio}-N'-2-(substituted phenyl) hydrazide with chloroacetylchloride were carried out in DMF-benzene solvent in the presence of Et(3)N catalyst. The microwave synthesis route afforded better yield with short time. The novel heterocycles were characterized by elemental analysis and spectral features. Some of the produced compounds were screened for their antimicrobial activity.

摘要

新型氮杂环丁烷-2-酮4a-j的高效快速合成方法已经确立。因此,在三乙胺催化剂存在下,2-{(1H-苯并咪唑)-基硫代}-N'-2-(取代苯基)酰肼与氯乙酰氯在N,N-二甲基甲酰胺-苯溶剂中进行了微波和传统缩合反应。微波合成路线在短时间内提供了更高的产率。通过元素分析和光谱特征对新型杂环化合物进行了表征。对部分生成的化合物进行了抗菌活性筛选。

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