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评价钌(II)-杂环卡宾配合物作为抗菌剂和细菌硫氧还蛋白还原酶抑制剂的作用。

Evaluation of Ruthenium(II) -Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase.

机构信息

Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, Beethovenstr. 55, 38106 Braunschweig, Germany.

Applied Microbiology, Faculty of Biology and Biotechnology, Ruhr University Bochum, Universitätsstr. 150, 44801 Bochum, Germany.

出版信息

Molecules. 2021 Jul 15;26(14):4282. doi: 10.3390/molecules26144282.

Abstract

A series of ruthenium(II) complexes with -heterocyclic carbene (NHC) ligands of the general type (arene)(NHC)Ru(II)X (where X = halide) was prepared, characterized, and evaluated as antibacterial agents in comparison to the respective metal free benzimidazolium cations. The ruthenium(II) NHC complexes generally triggered stronger bacterial growth inhibition than the metal free benzimidazolium cations. The effects were much stronger against Gram-positive bacteria ( and ) than against Gram-negative bacteria (,  , ), and all complexes were inactive against the fungus . Moderate inhibition of bacterial thioredoxin reductase was confirmed for selected complexes, indicating that inhibition of this enzyme might be a contributing factor to the antibacterial effects.

摘要

一系列钌(II)配合物,带有 -杂环卡宾(NHC)配体,通式为(芳基)(NHC)Ru(II)X(其中 X = 卤化物),已被制备、表征,并作为抗菌剂进行评估,与各自的金属自由苯并咪唑鎓阳离子进行比较。钌(II)NHC 配合物通常比金属自由苯并咪唑鎓阳离子引发更强的细菌生长抑制作用。这些作用对革兰氏阳性菌(和)比对革兰氏阴性菌(, ,)要强得多,所有配合物对真菌均无活性。对选定的配合物证实了中等抑制细菌硫氧还蛋白还原酶的作用,表明抑制这种酶可能是抗菌作用的一个因素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/327e/8303947/8aafddf37c6c/molecules-26-04282-sch001.jpg

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