新型巯基蛋白酶抑制剂的合成及构效关系

首都医科大学学报 ›› 2002, Vol. 23 ›› Issue (2): 107-109.

新型巯基蛋白酶抑制剂的合成及构效关系

陈改清¹, 何洁¹, 张枫¹, 李郁英², 李玉兰²

1. 首都医科大学化学教研室;2. 首都医科大学微生物教研室

收稿日期:2001-02-23 修回日期:1900-01-01 出版日期:2002-04-15 发布日期:2002-04-15

Synthesis and Structure-relationship of a New Kind of Inhibitor of Mercapto-proteinases

Chen Gaiqing¹, He Jie¹, Zhang Feng¹, Li Yuying², Li Yulan²

1. Department of Chemistry, Capital University of Medical Sciences;2. Department of Microbiology, Capital University of Medical Sciences

Received:2001-02-23 Revised:1900-01-01 Online:2002-04-15 Published:2002-04-15

摘要/Abstract

摘要： 对一类新的抗生素,即含有四氢-2H-1,3,5-噻二嗪-2-硫酮(tetrahydro2H-1,3,5-thiadiazine2-thione,THTT)环的化合物进行研究。根据其基本药效结构,该类抗生素的抗菌活性强弱主要取决于C₃位取代基,故设计在C₃位进行不同基团取代,共设计了14种3-取代-5-丝氨酸-四氢-2H-1,3,5-噻二嗪-2-硫酮化合物,经文献检索均未见报道,可视为新型化合物。化合物的化学结构经熔点测定、元素分析法、紫外光谱、红外光谱、¹H-磁共振加以确定。抗菌活性采用微生物敏感实验进行测定。体外抑菌实验表明,大部分化合物对所选常见致病菌有较好的活性及抗菌谱,特别是苄基取代的化合物,其初步的体外抑菌活性优于阳性对照磺胺嘧啶钠,提示对该类化合物值得进一步深入研究。

关键词: 抗菌活性, 噻二嗪硫酮, 构效关系

Abstract: A new kind of antibiotics containing Tetrahydro-2H-1,3,5-thiadiazine-2-thione(THTT)was studied. According to the basic structure-relationship of THTT, the antimicrobial activity is mainly depended on the C₃-substituents. The structure of these compounds were confirmed by UV, IR, H-NMR and elemental analysis. The in vitro activity of the compounds against 6 kinds of bacteria was tested. The antimicrobial activities of all compounds were more potent than sulfadiazine sodium, especially the benzal-substituent THTT, which suggest that it may be worth studying further.

Key words: antimicrobial activities|thiadiazine-2-thione|structure-activity relation

中图分类号:

R914

陈改清;何洁;张枫;李郁英;李玉兰. 新型巯基蛋白酶抑制剂的合成及构效关系[J]. 首都医科大学学报, 2002, 23(2): 107-109.

Chen Gaiqing;He Jie;Zhang Feng;Li Yuying;Li Yulan. Synthesis and Structure-relationship of a New Kind of Inhibitor of Mercapto-proteinases[J]. Journal of Capital Medical University, 2002, 23(2): 107-109.

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