• 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

合成及药理评价新型系列 3-芳基-2-(2-取代-4-甲基噻唑-5-基)噻唑烷-4-酮作为潜在的抗炎和抗菌药物。

Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents.

机构信息

Department of Chemistry, HPT Arts and RYK Science College, Vidyanagari, Nashik 422005, India.

出版信息

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6373-6. doi: 10.1016/j.bmcl.2012.08.073. Epub 2012 Aug 25.

DOI:10.1016/j.bmcl.2012.08.073
PMID:22981329
Abstract

A new series of 3-aryl-2-(2-aryl/benzyl-4-methylthiazole-5-yl)thiazolidin-4-one was synthesized by condensation of 2-aryl/benzyl-4-methylthiazole-5-carbaldehyde, aromatic amines and thioglycolic acid in toluene. All the synthesized compounds are characterized by IR, NMR and elemental or mass analysis. Sixteen out of the newly synthesized compounds were screened for in vivo anti-inflammatory activity using carrageenan-induced rat paw edema method. Some of the synthesized compounds exhibited good anti-inflammatory activity compared with indomethacin. The synthesized compounds were also evaluated for their in vitro antimicrobial activity. Some of the compounds showed mild antibacterial activity while most of the compounds showed good antifungal activity.

摘要

通过 2-芳基/苄基-4-甲基噻唑-5-甲醛、芳香胺和巯基乙酸在甲苯中的缩合反应,合成了一系列新的 3-芳基-2-(2-芳基/苄基-4-甲基噻唑-5-基)噻唑烷-4-酮。所有合成的化合物均通过 IR、NMR 和元素或质量分析进行了表征。十六种新合成的化合物通过角叉菜胶诱导的大鼠足肿胀法进行了体内抗炎活性筛选。与吲哚美辛相比,一些合成的化合物表现出良好的抗炎活性。还评估了合成化合物的体外抗菌活性。一些化合物表现出轻微的抗菌活性,而大多数化合物表现出良好的抗真菌活性。

相似文献

1
Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents.合成及药理评价新型系列 3-芳基-2-(2-取代-4-甲基噻唑-5-基)噻唑烷-4-酮作为潜在的抗炎和抗菌药物。
Bioorg Med Chem Lett. 2012 Oct 15;22(20):6373-6. doi: 10.1016/j.bmcl.2012.08.073. Epub 2012 Aug 25.
2
Design, synthesis, and evaluation of thiazolidinone derivatives as antimicrobial and anti-viral agents.噻唑烷酮衍生物的设计、合成及作为抗菌和抗病毒药物的评价。
Chem Biol Drug Des. 2011 Sep;78(3):464-70. doi: 10.1111/j.1747-0285.2011.01149.x. Epub 2011 Jul 8.
3
Synthesis, antimicrobial and anti-inflammatory activities of some 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines bearing trichlorophenyl moiety.一些带有三氯苯基部分的1,2,4-三唑并[3,4-b][1,3,4]噻二唑和1,2,4-三唑并[3,4-b][1,3,4]噻二嗪的合成、抗菌及抗炎活性
Eur J Med Chem. 2008 Apr;43(4):808-15. doi: 10.1016/j.ejmech.2007.06.026. Epub 2007 Jul 17.
4
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.1H-吡唑的一些噻唑基和噻二唑基衍生物作为抗炎抗菌剂的合成及生物学评价
Eur J Med Chem. 2008 Mar;43(3):456-63. doi: 10.1016/j.ejmech.2007.03.030. Epub 2007 Apr 14.
5
Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents.设计、合成一些新的(2-氨基噻唑-4-基)甲酯衍生物作为可能的抗菌和抗结核药物。
Eur J Med Chem. 2012 Mar;49:172-82. doi: 10.1016/j.ejmech.2012.01.008. Epub 2012 Jan 12.
6
Synthesis and biological evaluation of some 5-arylidene-2-(1,3-thiazol-2-ylimino)-1,3-thiazolidin-4-ones as dual anti-inflammatory/antimicrobial agents.一些 5-芳基-2-(1,3-噻唑-2-亚基氨基)-1,3-噻唑烷-4-酮的合成及生物评价作为双重抗炎/抗菌剂。
Bioorg Med Chem. 2013 Jan 15;21(2):532-9. doi: 10.1016/j.bmc.2012.10.046. Epub 2012 Nov 17.
7
Synthesis and biological evaluation of some pyrazolylpyrazolines as anti-inflammatory-antimicrobial agents.合成及某些吡唑并吡唑啉类化合物的抗炎抗菌活性评价。
Eur J Med Chem. 2010 Jun;45(6):2650-5. doi: 10.1016/j.ejmech.2010.01.059. Epub 2010 Jan 29.
8
Synthesis and biological evaluation of a novel series of 2,2-bisaminomethylated aurone analogues as anti-inflammatory and antimicrobial agents.新型 2,2-双氨甲基化黄酮类似物的合成及抗炎抗菌活性评价。
Eur J Med Chem. 2010 Jul;45(7):3223-7. doi: 10.1016/j.ejmech.2010.03.045. Epub 2010 Apr 3.
9
Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents.新型(E)-1-(4-甲基-2-(烷基氨基)噻唑-5-基)-3-芳基丙烯-1-酮类化合物作为有效的抗菌剂。
Bioorg Med Chem. 2011 Dec 15;19(24):7349-56. doi: 10.1016/j.bmc.2011.10.059. Epub 2011 Oct 25.
10
Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent.合成和黄酮哌嗪衍生物的生物评价作为潜在的抗炎和抗菌剂。
Bioorg Med Chem Lett. 2012 Oct 15;22(20):6385-90. doi: 10.1016/j.bmcl.2012.08.071. Epub 2012 Aug 24.

引用本文的文献

1
Biochemical evaluation of novel thiazolone derivatives as dual α-glucosidase/α-amylase inhibitors, anti-inflammatory agents.新型噻唑啉酮衍生物作为双功能α-葡萄糖苷酶/α-淀粉酶抑制剂及抗炎剂的生化评价
Future Med Chem. 2025 Jan;17(2):209-219. doi: 10.1080/17568919.2024.2447225. Epub 2024 Dec 29.
2
Recent advances in synthetic strategies and SAR of thiazolidin-4-one containing molecules in cancer therapeutics.含噻唑烷-4-酮结构的分子在癌症治疗中的合成策略和 SAR 的最新进展。
Cancer Metastasis Rev. 2023 Sep;42(3):847-889. doi: 10.1007/s10555-023-10106-1. Epub 2023 May 19.
3
Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.
发现并鉴定抗甲氧西林和万古霉素耐药金黄色葡萄球菌的噻唑类化合物。
J Med Chem. 2014 Feb 27;57(4):1609-15. doi: 10.1021/jm401905m. Epub 2014 Jan 14.