Synthesis of New Oxindoles and Determination of Their Antibacterial Properties

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2020-02-08 DOI:10.1155/2020/8021920

P. Romo, B. Insuasty, R. Abonía, M. Crespo, J. Quiroga

引用次数: 4

Abstract

A versatile method for the synthesis of new oxindoles was developed by the reaction between substituted isatins and 5-aminopyrazoles. The reaction was carried out at room temperature in ethanol using p-toluenesulfonic acid as the catalyst. The products were obtained with acceptable to excellent yields (44–96%). Structures of the new compounds were unambiguously established by spectroscopic and analytical techniques. The antibacterial activity was determined by microdilution assays. Compounds 3b, 3e, and 3g showed antistaphylococcal activity, particularly compound 3e displayed a potent activity against the vancomycin intermediate Staphylococcus aureus (VISA). Compounds 3i, 3j, and 3o inhibited Neisseria gonorrhoeae growth.

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新型环氧化合物的合成及其抗菌性能的测定

通过取代的靛蓝与5-氨基吡唑的反应，开发了一种合成新的羟吲哚的通用方法。反应在室温下在乙醇中使用对甲苯磺酸作为催化剂进行。产物以可接受的优异产率（44–96%）获得。通过光谱和分析技术明确地确定了新化合物的结构。通过微量稀释法测定抗菌活性。化合物3b、3e和3g显示出抗葡萄球菌活性，特别是化合物3e显示出对万古霉素中间体金黄色葡萄球菌（VISA）的有效活性。化合物3i、3j和3o抑制淋病奈瑟菌的生长。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.