药学学报2024,Vol.59Issue(1) :161-165.DOI:10.16438/j.0513-4870.2023-0790

含氨基噻唑肟结构的膦酸酯衍生物的合成与抗菌活性研究

Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment

陈阳密 安艳 董向涛 卢子聪 杨家强
药学学报2024,Vol.59Issue(1) :161-165.DOI:10.16438/j.0513-4870.2023-0790

含氨基噻唑肟结构的膦酸酯衍生物的合成与抗菌活性研究

Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment

陈阳密 1安艳 1董向涛 1卢子聪 1杨家强1
扫码查看

作者信息

  • 1. 遵义医科大学药学院,贵州遵义 563000
  • 折叠

摘要

采用分子杂合原理,将氨基噻唑肟与膦酸酯片段组合,设计合成了 15个目标物进行抗菌活性研究.结果显示:该类衍生物对所测试细菌有较好的抑制作用,尤以化合物Ⅲf和Ⅲi的抗金葡菌(S.aureus)、大肠杆菌(E.coli)、耐甲氧西林金葡菌(MRSA)和耐氟喹诺酮大肠杆菌(FREC)活性最为显著,前者的最小抑菌浓度(MIC)分别为1、8、4和16 μg·mL-1,后者的MIC分别为4、4、16和8 μg·mL-1,抗S.aureus活性略低于苯唑西林,抗E.coli、MRSA和FREC活性优于对照药苯唑西林,值得进一步深入研究.

Abstract

Based on the principle of molecular hybridization,fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment.The results showed that these compounds had better inhibitory effects on the tested bacteria.In particular,the activities of compounds Ⅲf and Ⅲi against S.aureus,E.coli,methicillin-resistant S.aureus(MRSA)and fluoroquinolone-resistant E.coli(FREC)were the most significant,the minimal inhibitory concentration(MIC)of Ⅲf was 1,8,4,16 μg·mL-1 respectively,and the MIC of Ⅲi was 4,4,16,8 μg·mL-1 respectively,which were slightly lower than that of the control drug oxacillin,and their anti-E.coli,MRSA and FREC activities were superior to that of the control drug oxacillin.Their activities to S.aureus were close to that of oxacillin,and to E.coli,MRSA and FREC were superior to that of oxacillin,which is worthy of further study.

关键词

氨基噻唑肟/膦酸酯/分子杂合/合成/抗菌活性

Key words

aminothiazole oxime/phosphonate/molecular hybridization/synthesis/antibacterial activity

引用本文复制引用

基金项目

贵州省科技厅国际合作项目(黔科合外G字[2014]7013)

遵义市科技计划(遵市科合HZ字[2020]41号)

出版年

2024
药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCD北大核心
影响因子:1.274
ISSN:0513-4870
参考文献量18
段落导航相关论文