靛红衍生唑类化合物作为新型潜在抗菌剂的设计、合成与生物评价。
Isatin-derived azoles as new potential antimicrobial agents: Design, synthesis and biological evaluation.
机构信息
Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, PR China.
Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Luminescence Analysis and Molecular Sensing, Ministry of Education, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, PR China.
出版信息
Bioorg Med Chem Lett. 2021 Jun 1;41:128030. doi: 10.1016/j.bmcl.2021.128030. Epub 2021 Apr 8.
Novel antibiotics are forced to be developed on account of multidrug-resistant bacteria with serious threats to human health. This work developed isatin-derived azoles as new potential antimicrobial agents. Bioactive assay revealed that isatin hybridized 1,2,4-triazole 7a exhibited excellent inhibitory activity against E. coli ATCC 25,922 with an MIC value of 1 µg/mL, which was 8-fold more potent than reference drug norfloxacin. The active molecule 7a possessed the ability to kill some bacteria and fungi as well as displayed low propensity to induce resistance towards E. coli ATCC25922. Preliminary mechanism investigation indicated that hybrid 7a might block deoxyribonucleic acid (DNA) replication by intercalating with DNA and possibly interacting with DNA polymerase III, thus exerting its antimicrobial potency.
新型抗生素的开发是由于具有严重威胁人类健康的多药耐药菌而迫不得已的。本工作开发了色酮衍生的唑类化合物作为新型潜在抗菌药物。生物活性测定表明，色酮与 1,2,4-三唑 7a 杂交后，对大肠杆菌 ATCC 25922 的抑制活性非常出色，MIC 值为 1μg/mL，比参考药物诺氟沙星强 8 倍。活性分子 7a 不仅具有杀灭某些细菌和真菌的能力，而且对大肠杆菌 ATCC25922 的耐药性诱导倾向也较低。初步的机制研究表明，杂合体 7a 可能通过与 DNA 相互作用并可能与 DNA 聚合酶 III 相互作用来阻止 DNA 复制，从而发挥其抗菌作用。
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