关键词: 硫肽, 噻肟酰胺衍生物, 药物设计, 合成, 抗菌活性

Abstract: In order to obtain novel antibacterial compounds, using the principle of pharmacophore assembly, twenty-four novel thioxime amide derivatives containing thiopeptide were designed and synthesized by combining active fragments of amino thiazole, oxime and thiopeptides, and confirmed by means of nuclear magnetic resonance hydrogen spectroscopy(1H NMR), nuclear magnetic resonance carbon spectroscopy(13C NMR) and elemental analysis. The antibacterial activities test results showed that these derivatives have significant activity against Gram positive bacteria. the minimum inhibitory concentration(MIC) values of compound 5u against S. aureus and methicillin-resistant S. aureus(MRSA) were 0.25 μg/mL and 2 μg/mL respectively, the MIC values of 5v against S. aureus and MRSA were 0.5 μg/mL and 2 μg/mL, respectively. Its anti- S. aureus activity was superior to that of the control drug oxacillin(MIC=0.5 μg/mL) or relatively, and its anti-MRSA activity was significantly better than that of the control drug(MIC＞128 μg/mL), which will be further developed as novel candidates for antibacterial drugs.

Key words: Thiopeptide; Thioxime amide derivatives, Drug design, Synthesis, Antibacterial activity