Assessment of the biological potential of diaryltriazene-derived triazene compounds

• Published in: Scientific reports 2021-01, Vol.11 (1), p.2541-15, Article 2541
• Main Authors: Figueirêdo, Patricia de Maria Silva, Sampaio Filho, José Costa, Sodré, Alzirene de Jesus Sales, de Castro Júnior, José Ribamar, Gonçalves, Ingrid Santos, Blasques, Rodrigo Vieira, S. Correa, Rodrigo, Lima, Benedicto Augusto Vieira, dos Anjos Marques, Larissa, Coutinho, Denise Fernandes, de Azevedo dos Santos, Ana Paula Silva, Luz, Tássio Rômulo Silva Araújo, de Miranda, Rita de Cassia Mendonça, dos Santos, Julliana Ribeiro Alves, Doriguetto, Antonio Carlos, Pividori, María Isabel, Hörner, Manfredo, Villis, Paulo Cesar Mendes
• Format: Article
• Language: English
• Subjects: 631/154; 631/326; 639/638; Alkylating agents; American Type Culture Collection; Antibiotics; Antifungal activity; Antimicrobial agents; Bacteria; Biological activity; Cancer; Chemistry; Clinical isolates; Cytotoxicity; Drug resistance; Fungi; Gram-negative bacteria; Humanities and Social Sciences; Microorganisms; Minimum inhibitory concentration; multidisciplinary; NMR; Nuclear magnetic resonance; Physicochemical properties; Science; Science (multidisciplinary); Sensitivity analysis; Staphylococcus infections; Yeasts
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/s41598-021-81823-2

In the present study, novel, 1,3-diaryltriazene-derived triazene compounds were synthesized and tested. Triazenes are versatile and belong to a group of alkylating agents with interesting physicochemical properties and proven biological activities. This study describes the synthesis, molecular and crystalline structure, biological activity evaluation, and antifungal and antimicrobial potentials of 1,3- bis (X-methoxy-Y-nitrophenyl)triazenes [X = 2 and 5; Y = 4 and 5]. The antimicrobial and antifungal activities of the compounds were tested by evaluating the sensitivity of bacteria (American Type Culture Collection, ATCC) and clinical isolates to their solutions using standardized microbiological assays, cytotoxicity evaluation, and ecotoxicity tests. The antimicrobial potentials of triazenes were determined according to their minimum inhibitory concentrations (MICs); these compounds were active against gram-positive and gram-negative bacteria, with low MIC values. The most surprising result was obtained for T3 having the effective MIC of 9.937 µg/mL and antifungal activity against Candida albicans ATCC 90028, C. parapsilosis ATCC 22019, and C. tropicallis IC. To the best of our knowledge, this study is the first to report promising activities of triazene compounds against yeast and filamentous fungi. The results showed the potential utility of triazenes as agents affecting selected resistant bacterial and fungal strains.