Access to a library of 1,3-disubstituted-1,2,3-triazenes and evaluation of their antimicrobial properties

Insa Seck, Samba Fama Ndoye, Lalla Aicha Ba, Alioune Fall, Abdoulaye Diop, Ismaïla Ciss, Abda Ba, Cheikh Sall, Amadou Diop, Cheikh Sadibou Boye, Generosa Gomez, Yagamare Fall, Matar Seck

Research output: Contribution to journalArticlepeer-review

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. 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.

Original languageEnglish
Pages (from-to)713-719
Number of pages7
JournalCurrent Topics in Medicinal Chemistry
Volume20
Issue number9
DOIs
Publication statusPublished - 1 Jan 2020
Externally publishedYes

Keywords

  • Antimicrobial
  • Minimal inhibitory concentrations
  • Resistance
  • Strains
  • Triazene

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