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Synthesis of New Oxindoles and Determination of Their Antibacterial Properties
Heteroatom Chemistry ( IF 1.1 ) Pub Date : 2020-02-08 , DOI: 10.1155/2020/8021920
Pablo E. Romo 1 , Braulio Insuasty 1 , Rodrigo Abonia 1 , María del Pilar Crespo 2 , Jairo Quiroga 1
Affiliation  

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.

中文翻译:

新型羟吲哚的合成及其抗菌性能的测定

通过取代靛红和 5-氨基吡唑之间的反应,开发了一种合成新羟吲哚的通用方法。反应在室温下在乙醇中使用对甲苯磺酸作为催化剂进行。获得的产品具有可接受到极好的收率(44-96%)。通过光谱和分析技术明确确定了新化合物的结构。抗菌活性通过微量稀释测定法测定。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。
更新日期:2020-02-08
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