Résumé
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. Method: 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 Pseudo-monas aeruginosa and 0.64 µM against Enterococcus faecalis and Pseudomonas aeruginosa. Conclusion: Comparing the structure activity relationship, electron withdrawing groups appear to in-crease antimicrobial activity.
| langue originale | Anglais |
|---|---|
| Pages (de - à) | 713-719 |
| Nombre de pages | 7 |
| journal | Current Topics in Medicinal Chemistry |
| Volume | 20 |
| Numéro de publication | 9 |
| Les DOIs | |
| état | Publié - 1 janv. 2020 |
| Modification externe | Oui |
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