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评估二芳基三氮烯衍生的三氮烯类化合物的生物潜力。

Assessment of the biological potential of diaryltriazene-derived triazene compounds.

机构信息

Laboratório de Microbiologia Clínica, Federal University of Maranhão (UFMA), São Luís, MA, 65.080-040, Brazil.

Electrochemistry and Biotechnology Laboratory (EBL), University of CEUMA (UNICEUMA), São Luís, MA, 65.065-470, Brazil.

出版信息

Sci Rep. 2021 Jan 28;11(1):2541. doi: 10.1038/s41598-021-81823-2.

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.

摘要

在本研究中,合成并测试了新型 1,3-二芳基三嗪衍生的三嗪化合物。三嗪是多功能的,属于一组具有有趣物理化学性质和已证明生物活性的烷化剂。本研究描述了 1,3-双(X-甲氧基-Y-硝基苯基)三嗪[X = 2 和 5;Y = 4 和 5]的合成、分子和晶体结构、生物活性评价以及抗真菌和抗菌潜力。通过使用标准化微生物测定法、细胞毒性评估和生态毒性测试来评估化合物溶液对细菌(美国模式培养物集存库,ATCC)和临床分离株的敏感性,测试了这些化合物的抗菌和抗真菌活性。根据最小抑菌浓度(MICs)确定了三嗪的抗菌潜力;这些化合物对革兰氏阳性和革兰氏阴性细菌均具有活性,MIC 值较低。最令人惊讶的结果是 T3 获得了有效的 MIC 为 9.937 µg/mL 的活性,对 Candida albicans ATCC 90028、C. parapsilosis ATCC 22019 和 C. tropicallis IC 具有抗真菌活性。据我们所知,这项研究首次报道了三嗪化合物对酵母和丝状真菌的有希望的活性。结果表明,三嗪具有作为影响所选耐药细菌和真菌菌株的试剂的潜在用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/93b1/7844262/f90be54ea67e/41598_2021_81823_Fig1_HTML.jpg

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