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新型抗菌碘代二氢吡咯-2-酮化合物

Novel antimicrobial iodo-dihydro-pyrrole-2-one compounds.

作者信息

Al-Matarneh Cristina M, Nicolescu Alina, Marinas Ioana C, Chifiriuc Mariana C, Shova Sergiu, Silion Mihaela, Pinteala Mariana

机构信息

Research Institute of the University of Bucharest-ICUB, 91-95 Spl. Independentei, Bucharest, 050095, Romania.

Center of Advanced Research in Bionanoconjugates & Biopolymers, "Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, 41A Grigore Ghica Voda Alley, Iasi, 700487, Romania.

出版信息

Future Med Chem. 2023 Aug;15(15):1369-1391. doi: 10.4155/fmc-2023-0121. Epub 2023 Aug 14.

Abstract

A series of new hybrid molecules with two iodine atoms on the sides were synthesized. A one-pot, two-component method with trifluoroacetic acid as an effective catalyst to obtain dihydro-pyrrol-2-one compounds was developed. Short reaction times, a cheap catalyst, high yields and clean work-up are benefits of this method. The chemical structures of the newly synthesized compounds were verified through spectroscopic techniques. Their antimicrobial activity against , and was tested . NC- and OH- radicals confer broad-spectrum antimicrobial activity, including against Gram-positive and Gram-negative bacteria and yeasts. Compounds > and > were most active on the two bacterial species, while > and > were most active against the fungal strain.

摘要

合成了一系列在两侧带有两个碘原子的新型杂化分子。开发了一种以三氟乙酸为有效催化剂的一锅法双组分方法来制备二氢吡咯-2-酮化合物。该方法具有反应时间短、催化剂便宜、产率高和后处理简便等优点。通过光谱技术验证了新合成化合物的化学结构。测试了它们对[此处原文缺失具体测试对象]、[此处原文缺失具体测试对象]和[此处原文缺失具体测试对象]的抗菌活性。NC-和OH-自由基具有广谱抗菌活性,包括对革兰氏阳性菌、革兰氏阴性菌和酵母。化合物[此处原文缺失具体化合物编号]>和[此处原文缺失具体化合物编号]>对这两种细菌最具活性,而[此处原文缺失具体化合物编号]>和[此处原文缺失具体化合物编号]>对真菌菌株最具活性。

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