抗菌剂
肉汤微量稀释
金黄色葡萄球菌
化学
最小抑制浓度
抗菌活性
表皮葡萄球菌
生物利用度
微生物学
毛癣菌
细菌
生物
有机化学
抗真菌
药理学
遗传学
作者
Melese Legesse,Abiy Abebe,Sileshi Degu,Yonatan Alebachew,Solomon Tadesse
标识
DOI:10.1080/14786419.2022.2139696
摘要
In the present study, we use knipholone as a prototype molecule to identify new anti-infective agents. Since knipholone is insoluble in water, which would have a detrimental effect on its bioavailability and efficacy, we synthesized knipholone Mannich base derivatives (2-4) that have better predicted solubility and investigated their in vitro antimicrobial activity against eight pathogenic bacterial and fungal strains. The chemical structures of compounds 1-4 were elucidated from their 1H and 13C NMR data, and their antimicrobial activity evaluation was carried out by a broth microdilution MTT assay. Compound 3 exhibited the strongest efficacy against Staphylococcus epidermidis, with MIC value of 9.7 µg/mL. While 4 exhibited the best activity against Staphylococcus aureus, with an MIC value of 19.5 µg/mL, and was the only one to significantly inhibit the fungus Trichophyton mentagrophytes (MIC = 78.2 µg/mL). The study provides evidence for the antibacterial activity of aminoalkyl derivatives of knipholone.
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