Ungureanu Daniel, Oniga Ovidiu, Moldovan Cristina, Ionuț Ioana, Marc Gabriel, Stana Anca, Pele Raluca, Duma Mihaela, Tiperciuc Brîndușa
Department of Pharmaceutical Chemistry, "Iuliu Hațieganu" University of Medicine and Pharmacy, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania.
"Prof. Dr. Ion Chiricuță" Oncology Institute, 34-36 Republicii Street, 400015 Cluj-Napoca, Romania.
Antibiotics (Basel). 2024 Aug 13;13(8):763. doi: 10.3390/antibiotics13080763.
Antimicrobial resistance poses a major threat to global health as the number of efficient antimicrobials decreases and the number of resistant pathogens rises. Our research group has been actively involved in the design of novel antimicrobial drugs. The blueprints of these compounds were azolic heterocycles, particularly thiazole. Starting with oxadiazolines, our research group explored, one by one, the other five-membered heterocycles, developing more or less potent compounds. An overview of this research activity conducted by our research group allowed us to observe an evolution in the methodology used (from inhibition zone diameters to minimal inhibitory concentrations and antibiofilm potential determination) correlated with the design of azole compounds based on results obtained from molecular modeling. The purpose of this review is to present the development of in-house azole compounds with antimicrobial activity, designed over the years by this research group from the departments of Pharmaceutical and Therapeutical Chemistry in Cluj-Napoca.
随着有效抗菌药物数量的减少和耐药病原体数量的增加，抗菌药物耐药性对全球健康构成了重大威胁。我们的研究小组一直积极参与新型抗菌药物的设计。这些化合物的蓝本是唑类杂环，特别是噻唑。从恶二唑啉开始，我们的研究小组逐一探索了其他五元杂环，开发出了或多或少具有活性的化合物。对我们研究小组开展的这项研究活动进行概述后，我们观察到所使用的方法（从抑菌圈直径到最低抑菌浓度和抗生物膜潜力测定）发生了演变，这与基于分子建模结果设计的唑类化合物相关。本综述的目的是介绍多年来由克卢日-纳波卡制药与治疗化学系的这个研究小组设计的具有抗菌活性的内部唑类化合物的研发情况。
