• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

抗结核药物的定向开发（第二部分）：卤代3-(4-烷基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮

The oriented development of antituberculotics (Part II): halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones.

作者信息

Waisser Karel, Matyk Josef, Divisová Hana, Husáková Petra, Kunes Jirí, Klimesová Vera, Palát Karel, Kaustová Jarmila

机构信息

Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Heyrovského, Czech Republic.

出版信息

Arch Pharm (Weinheim). 2007 May;340(5):264-7. doi: 10.1002/ardp.200600002.

DOI:10.1002/ardp.200600002
PMID:17516578
Abstract

Based on our previous studies, 21 new halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones were synthesized by the reaction of salicylanilides and methyl-chloroformate. All compounds were screened in vitro against three different strains of mycobacterium, and Free-Wilson method was used to establish structure-activity relationships. 6-Bromo-3-(4-butylphenyl)-1,3-benzoxazine-2,4-(3H)-dione 3b proved to be the most active compound of the series.

摘要

基于我们之前的研究，通过水杨酰苯胺与氯甲酸甲酯反应合成了21种新型卤代3-(4-烷基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮。所有化合物均针对三种不同的分枝杆菌菌株进行了体外筛选，并采用Free-Wilson方法建立构效关系。6-溴-3-(4-丁基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮3b被证明是该系列中活性最高的化合物。

相似文献

1
The oriented development of antituberculotics (Part II): halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones.抗结核药物的定向开发（第二部分）：卤代3-(4-烷基苯基)-1,3-苯并恶嗪-2,4-(3H)-二酮
Arch Pharm (Weinheim). 2007 May;340(5):264-7. doi: 10.1002/ardp.200600002.
2
The oriented development of antituberculotics: salicylanilides.抗结核药物的定向开发：水杨酰苯胺类
Arch Pharm (Weinheim). 2006 Nov;339(11):616-20. doi: 10.1002/ardp.200600093.
3
[Antimicrobial salicylanilides and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones].[抗微生物水杨酰苯胺类和3-苯基-2H-1,3-苯并恶嗪-2,4(3H)-二酮]
Ceska Slov Farm. 2001 May;50(3):148-52.
4
Highly active potential antituberculotics: 3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dihiones substituted in ring-B by halogen.高活性潜在抗结核药物：3-(4-烷基苯基)-4-硫代-2H-1,3-苯并恶嗪-2(3H)-酮和在B环上被卤素取代的3-(4-烷基苯基)-2H-1,3-苯并恶嗪-2,4(3H)-二酮
Arch Pharm (Weinheim). 2008 Dec;341(12):800-3. doi: 10.1002/ardp.200800004.
5
Relationships between the chemical structure of antimycobacterial substances and their activity against atypical strains. Part 14: 3-Aryl-6,8-dihalogeno-2H-1,3-benzoxazine-2,4(3H)-diones.抗分枝杆菌物质的化学结构与其对非典型菌株活性之间的关系。第14部分：3-芳基-6,8-二卤代-2H-1,3-苯并恶嗪-2,4(3H)-二酮
Arch Pharm (Weinheim). 1998 Jan;331(1):3-6. doi: 10.1002/(sici)1521-4184(199801)331:1<3::aid-ardp3>3.0.co;2-2.
6
Highly active antimycobacterial derivatives of benzoxazine.具有高抗分枝杆菌活性的苯并恶嗪衍生物。
Bioorg Med Chem. 2010 Dec 1;18(23):8178-87. doi: 10.1016/j.bmc.2010.10.017. Epub 2010 Oct 19.
7
Influence of the replacement of the oxo function with the thioxo group on the antimycobacterial activity of 3-aryl-6,8-dichloro-2H-1,3-benzoxazine-2,4(3H)-diones and 3-arylquinazoline-2,4(1H,3H)-diones.用硫代羰基取代氧代官能团对3-芳基-6,8-二氯-2H-1,3-苯并恶嗪-2,4(3H)-二酮和3-芳基喹唑啉-2,4(1H,3H)-二酮抗分枝杆菌活性的影响。
Farmaco. 2001 Oct;56(10):803-7. doi: 10.1016/s0014-827x(01)01134-x.
8
Relationship between the structure and antimycobacterial activity of substituted salicylanilides.取代水杨酰苯胺的结构与抗分枝杆菌活性之间的关系。
Arch Pharm (Weinheim). 2003 Mar;336(1):53-71. doi: 10.1002/ardp.200390004.
9
[New groups of potential antitubercular agents: 3-(4-ethoxythiocarbonylphenyl)-2-H-benzoxazin-2,4(3H)-diones and 3-(4-ethoxythiocarbonylphenyl)-4-thioxy-2H-benzoxazin-2(3H)-ones].新型潜在抗结核药物：3-(4-乙氧基硫代羰基苯基)-2-H-苯并恶嗪-2,4(3H)-二酮和3-(4-乙氧基硫代羰基苯基)-4-硫氧基-2H-苯并恶嗪-2(3H)-酮
Ceska Slov Farm. 2003 Jan;52(1):42-7.
10
Antimycobacterial 3-aryl-2H-1,3-benzoxazine-2,4(3H)-diones.抗分枝杆菌的3-芳基-2H-1,3-苯并恶嗪-2,4(3H)-二酮
Pharmazie. 2003 Feb;58(2):83-94.

引用本文的文献

1
Encapsulation of progesterone in reishi mushroom composite for optimized hormone replacement and targeted anticancer therapy.将孕酮封装在灵芝复合物中以实现优化的激素替代和靶向抗癌治疗。
RSC Adv. 2025 Jun 20;15(24):19392-19416. doi: 10.1039/d5ra02368h. eCollection 2025 Jun 4.
2
Synthesis of 3,5-isoxazolidinediones and 1H-2,3-benzoxazine-1,4(3H)-diones from aliphatic oximes and dicarboxylic acid chlorides.由脂肪族肟和二羧酸氯化物合成3,5-异恶唑烷二酮和1H-2,3-苯并恶嗪-1,4(3H)-二酮
J Org Chem. 2014 Apr 4;79(7):2874-82. doi: 10.1021/jo402708j. Epub 2014 Mar 21.