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两种5-硝基咪唑衍生物的体外研究。

In-vitro studies of two 5-nitroimidazole derivatives.

作者信息

Castelli M, Malagoli M, Ruberto A I, Baggio A, Casolari C, Cermelli C, Bossa M R, Rossi T, Paolucci F, Roffia S

机构信息

Department of Biomedical Sciences, Section of Pharmacology, University of Modena, Italy.

出版信息

J Antimicrob Chemother. 1997 Jul;40(1):19-25. doi: 10.1093/jac/40.1.19.

Abstract

This paper reports the findings obtained using two new compounds belonging to the 5-nitroimidazole family: sulphuridazole (V1) and sulphonidazole (V2). We first assessed their antimicrobial activity on Clostridia spp. and then extended the study to Gram-positive and Gram-negative aerobic microorganisms and to Candida albicans. Their MICs were compared with those of metronidazole. The findings show that the antibacterial and antimycotic activity of sulphonidazole is greater than that of sulphuridazole, while metronidazole is not active against any aerobic organism. It also emerges that the NO2 group is indispensable for all the microorganisms assayed and that sulphuridazole and sulphonidazole are the first two 5-nitroimidazoles active against C. albicans. The redox potentials of the 5-nitroimidozoles studied suggest that their action mechanism is mainly based on redox processes.

摘要

本文报道了使用两种属于5-硝基咪唑家族的新化合物:硫硝唑(V1)和磺硝唑(V2)所获得的研究结果。我们首先评估了它们对梭菌属的抗菌活性,然后将研究扩展到革兰氏阳性和革兰氏阴性需氧微生物以及白色念珠菌。将它们的最低抑菌浓度(MIC)与甲硝唑的MIC进行了比较。研究结果表明,磺硝唑的抗菌和抗真菌活性大于硫硝唑,而甲硝唑对任何需氧生物均无活性。还发现,对于所有检测的微生物,NO2基团都是必不可少的,并且硫硝唑和磺硝唑是最早对白色念珠菌有活性的两种5-硝基咪唑。所研究的5-硝基咪唑的氧化还原电位表明,它们的作用机制主要基于氧化还原过程。

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