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Synthesis, anti-ferroptosis, anti-quorum sensing, antibacterial and DNA interaction studies of chromene-hydrazone derivatives

化学 抗菌活性 组合化学 群体感应 DNA 立体化学 抗菌剂 化学合成 体外 生物化学 抗生素 细菌 基因 生物 毒力 遗传学
作者
Andrew J. Ressler,Marissa Frate,Ana Hontoria,Anna Ream,E. Timms,Huifang Li,Lauren D. Stettler,Ashton Bollinger,Jenna E. Poor,Michael A. Parra,Hang Ma,Navindra P. Seeram,Susan Meschwitz,Geneive E. Henry
出处
期刊:Bioorganic & Medicinal Chemistry [Elsevier]
卷期号:90: 117369-117369 被引量:5
标识
DOI:10.1016/j.bmc.2023.117369
摘要

Nineteen chromene-hydrazone derivatives containing a variety of structural modifications on the hydrazone moiety were synthesized. Structure-activity correlations were investigated to determine the influence of structural variations on anti-ferroptosis, anti-quorum sensing, antibacterial, DNA cleavage and DNA binding properties. Ferroptosis inhibitory activity was determined by measuring the ability of the derivatives to reverse erastin-induced ferroptosis. Several of the derivatives were more effective than fisetin at inhibiting ferroptosis, with the thiosemicarbazone derivative being the most effective. Quorum sensing inhibition was evaluated using Vibrio harveyi, and both V. harveyi and Staphylococcus aureus were used to determine antibacterial activity. The semicarbazone and benzensulfonyl hydrazone derivatives showed moderate quorum sensing inhibition with IC50 values of 27 μM and 22 μM, respectively, while a few aryl hydrazone and pyridyl hydrazone derivatives showed bacterial growth inhibition, with MIC values ranging from 3.9 to 125 μM. In addition, the interaction of the hydrazone derivatives with DNA was investigated by gel electrophoresis, UV-Vis spectroscopy and molecular docking. All of the derivatives cleaved plasmid DNA and showed favorable interaction with B-DNA through minor groove binding. Overall, this work highlights a broad range of pharmacological applications for chromene-hydrazone derivatives.

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