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新型2-(2-(4-取代基)乙酰胺基)-4-取代噻唑-5-羧酸乙酯衍生物的合成与抗菌活性评价

Synthesis and antimicrobial evaluation of novel ethyl 2-(2-(4-substituted)acetamido)-4-subtituted-thiazole-5-carboxylate derivatives.

作者信息

Pawar Chandrakant D, Sarkate Aniket P, Karnik Kshipra S, Bahekar Sushilkumar S, Pansare Dattatraya N, Shelke Rohini N, Jawale Chetan S, Shinde Devanand B

机构信息

Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, MS, India.

Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, MS, India.

出版信息

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3525-8. doi: 10.1016/j.bmcl.2016.06.030. Epub 2016 Jun 11.

Abstract

A series of novel molecules containing thiazole ring structure were designed and synthesized. The structures of the synthesized compounds were elucidated and confirmed by (1)H NMR, (13)C NMR, Mass spectrum and the purity was checked through HPLC analysis. Among these synthesized compounds, 3a-3i and 6a-6c were tested for their antimicrobial activity (minimum inhibitory concentration) against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus niger for antifungal activity respectively. The results of the antimicrobial screening data revealed that most of the tested compounds showed moderate to good microbial inhibitions.

摘要

设计并合成了一系列含有噻唑环结构的新型分子。通过¹H NMR、¹³C NMR、质谱对合成化合物的结构进行了阐明和确认,并通过高效液相色谱分析检查了纯度。在这些合成化合物中,分别测试了3a - 3i和6a - 6c对一系列枯草芽孢杆菌、金黄色葡萄球菌和大肠杆菌菌株的抗菌活性(最低抑菌浓度)以及对白色念珠菌、黄曲霉和黑曲霉菌株的抗真菌活性。抗菌筛选数据结果表明,大多数测试化合物表现出中度至良好的微生物抑制作用。

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