访问 1,3-二取代-1,2,3-三氮唑文库并评估其抗菌性能。

Access to a Library of 1,3-disubstituted-1,2,3-triazenes and Evaluation of their Antimicrobial Properties.

机构信息

Laboratoire de Chimie de Coordination Organique (LCCO), Departement de Chimie, Faculte des Sciences et Techniques, Universite Cheikh Anta Diop de Dakar, Dakar, Senegal.

Laboratoire de Chimie Organique et Therapeutique, Faculte de Medecine, de Pharmacie et d'Odontologie de l'Universite Cheikh Anta Diop de Dakar, BP 5005, Dakar- Fann, Senegal.

出版信息

Curr Top Med Chem. 2020;20(9):713-719. doi: 10.2174/1568026620666200127143005.

DOI:10.2174/1568026620666200127143005

PMID:31985378

Abstract

BACKGROUND

Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem.

OBJECTIVE

The objective of this work is to access 1,2,3-triazene-1,3-disubstituted, a class of molecule with high therapeutic potential.

METHODS

Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: two gram (-): Escherichia coli ATCC 25921 and Pseudomonas aeruginosa ATCC 27253; two gram (+) : Staphylococcus aureus ATCC 38213 and Enterococcus faecalis ATCC 29212; and one fungi: Candida albicans ATCC 24433.

RESULTS

All strains were sensitive and the best MIC, 0.28 µM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with satisfactory MIC 0.32 µM against Escherichia coli and Pseudomonas aeruginosa and 0.64 µM against Enterococcus faecalis and Pseudomonas aeruginosa.

CONCLUSION

Comparing the structure activity relationship, electron withdrawing groups appear to increase antimicrobial activity.

摘要

背景

由于微生物耐药性的迅速发展，寻找新的分子来对抗这一问题变得迫在眉睫。

目的

本工作旨在获得 1,2,3-三嗪-1,3-二取代物，这是一类具有高治疗潜力的分子。

方法

在这里，我们描述了对 17 种新三嗪的获得，包括 6 种含咪唑-1,2,3-三嗪部分和 11 种含烷基-1,2,3-三嗪部分，并对它们进行了针对五种菌株的评估：两种革兰氏阴性菌（-）：大肠杆菌 ATCC 25921 和铜绿假单胞菌 ATCC 27253；两种革兰氏阳性菌（+）：金黄色葡萄球菌 ATCC 38213 和粪肠球菌 ATCC 29212；以及一种真菌：白色念珠菌 ATCC 24433。