Synthesis, in vitro antibacterial activities of a series of 3-N-substituted canthin-6-ones.
Basic Information
ID: ALA3745648
Journal: Bioorg Med Chem Lett
Title: Synthesis, in vitro antibacterial activities of a series of 3-N-substituted canthin-6-ones.
Authors: Dai JK, Dan WJ, Li N, Du HT, Zhang JW, Wang JR.
Abstract: An improved synthetic route of canthin-6-one was accomplished. To further enhance the antibacterial potency and improve water solubility, a series of 3-N-alkylated and 3-N-benzylated canthin-6-ones were designed and synthesized, and their in vitro antibacterial activities were evaluated. A clear structure-activity relationship with peak minimal inhibitory concentration (MIC) values of 0.98 (μg·mL(-)(1)) was investigated. Particularly, compounds 6i-r and 6t were found to be the most potent compounds with minimal inhibitory concentration (MIC) values lower than 1.95 (μg·mL(-)(1)) against Staphylococcus aureus.
CiteXplore: 26681509
DOI: 10.1016/j.bmcl.2015.11.070
Patent ID: ┄