Department of Chemistry and Polymer Science, University of Stellenbosch, Stellenbosch, Private bag X1, Matieland, 7602, South Africa.
Molecular Science Institute, School of Chemistry, University of the Witwatersrand, Johannesburg, PO Wits, 2050, South Africa.
Chembiochem. 2023 Oct 4;24(19):e202300247. doi: 10.1002/cbic.202300247. Epub 2023 Sep 5.
Infections associated with antimicrobial resistance (AMR) are poised to become the leading cause of death in the next few decades, a scenario that can be ascribed to two phenomena: antibiotic over-prescription and a lack of antibiotic drug development. The crowd-sourced initiative Community for Open Antimicrobial Drug Discovery (CO-ADD) has been testing research compounds contributed by researchers around the world to find new antimicrobials to combat AMR, and during this campaign has found that metallodrugs might be a promising, yet untapped source. To this end, we submitted 18 Pd - and Ru -pyridyl-1,2,3-triazolyl complexes that were developed as catalysts to assess their antimicrobial properties. It was found that the Pd complexes, especially Pd1, possessed potent antifungal activity with MICs between 0.06 and 0.125 μg mL against Candida glabrata. The in-vitro studies were extended to in-vivo studies in Galleria mellonella larvae, where it was established that the compounds were nontoxic. Here, we effectively demonstrate the potential of Pd -pyta complexes as antifungal agents.
与抗菌药物耐药性（AMR）相关的感染将在未来几十年成为主要死因，这种情况可以归因于两个现象：抗生素过度处方和缺乏抗生素药物开发。众包倡议社区开放抗菌药物发现（CO-ADD）一直在测试世界各地研究人员贡献的研究化合物，以寻找新的抗菌药物来对抗 AMR，在此期间发现金属药物可能是一个有前途但尚未开发的来源。为此，我们提交了 18 种作为催化剂开发的 Pd-和 Ru-吡啶基-1,2,3-三唑基配合物，以评估它们的抗菌特性。结果发现，Pd 配合物，特别是 Pd1，对光滑念珠菌具有很强的抗真菌活性，MIC 值在 0.06 和 0.125 μg/mL 之间。体外研究扩展到了家蚕幼虫的体内研究，结果表明这些化合物没有毒性。在这里，我们有效地证明了 Pd-pyta 配合物作为抗真菌剂的潜力。
