【摘要】 以取代芳腈(杂环腈)为原料,经硫化、环化、酰胺化和环化反应合成了系列噻唑-噻唑啉骈合结构的杂环化合物。目标化合物经1H NMR、13C NMR和HRMS进行了结构确证。该路线后处理简单,环境友好,适合产业化生产。以大肠杆菌(Escherichia coli)、枯草芽孢杆菌(Bacillus subtilis)、金黄色葡萄球菌(Staphylococcus aureus)为测试对象,初步的生物活性测试结果表明,部分化合物具有一定的抗菌活性,其中5g,5i,5j对大肠杆菌(Escherichia coli)的抑制活性较强,5h,5i,5j对金黄色葡萄球菌(Staphylococcus aureus)的抑制活性较强,5b,5d对枯草芽孢杆菌(Bacillus subtilis)的抑制活性较强。更多还原

【Abstract】 A series of novel small molecules compounds with thiazoline and thiazole moiety of natural product largazole were designed and synthesized by salfuration,cyclization,amidation and cyclization.The structures of target compounds were characterized by1 H NMR,13 C NMR and MS spectra.The preliminary bioassay results revealed that some of the compounds were showing promising inhibitory activities against bacteria.Compounds 5 g,5 i and 5 j displayed stronger activity against E.coli.Compounds 5 h,5 i and 5 j demonstrated better activity against S.aureus,and 5 b,5 d had stronger inhibitory activity against B.subtilis.Primary structure-activity relationships( SARs) analysis indicated that furan or thiophene ting substituents in position-2 of thiazole were the suitable pharmacophoric group giving rise to better activity.更多还原