Assessment of the biological potential of diaryltriazene-derived triazene compounds

二芳基三氮烯衍生的三氮烯化合物的生物潜力评估

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作者:Patricia de Maria Silva Figueirêdo, José Costa Sampaio Filho, Alzirene de Jesus Sales Sodré, José Ribamar de Castro Júnior, Ingrid Santos Gonçalves, Rodrigo Vieira Blasques, Rodrigo S Correa, Benedicto Augusto Vieira Lima, Larissa Dos Anjos Marques, Denise Fernandes Coutinho, Ana Paula Silva de Azev

Abstract

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.

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