• 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

抗结核羧酰胺的合成及其构效关系研究

Synthesis and structural activity relationship study of antitubercular carboxamides.

作者信息

Ugwu D I, Ezema B E, Eze F U, Ugwuja D I

机构信息

Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka 410002, Nigeria.

Department of Chemical Sciences, Federal University, Wukari, Nigeria.

出版信息

Int J Med Chem. 2014;2014:614808. doi: 10.1155/2014/614808. Epub 2014 Dec 30.

DOI:10.1155/2014/614808
PMID:25610646
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4295614/
Abstract

The unusual structure and chemical composition of the mycobacterial cell wall, the tedious duration of therapy, and resistance developed by the microorganism have made the recurrence of the disease multidrug resistance and extensive or extreme drug resistance. The prevalence of tuberculosis in synergy with HIV/AIDS epidemic augments the risk of developing the disease by 100-fold. The need to synthesize new drugs that will shorten the total duration of effective treatment and/or significantly reduce the dosage taken under DOTS supervision, improve on the treatment of multidrug-resistant tuberculosis which defies the treatment with isoniazid and rifampicin, and provide effective treatment for latent TB infections which is essential for eliminating tuberculosis prompted this review. In this review, we considered the synthesis and structure activity relationship study of carboxamide derivatives with antitubercular potential.

摘要

分枝杆菌细胞壁异常的结构和化学成分、冗长的治疗周期以及微生物产生的耐药性，使得该疾病复发出现多重耐药和广泛或极度耐药情况。结核病的流行与艾滋病毒/艾滋病疫情协同作用，使患病风险增加了100倍。合成能够缩短有效治疗总时长和/或显著减少在直接观察治疗（DOTS）监督下服用剂量的新药，改进对耐异烟肼和利福平的耐多药结核病的治疗，并为潜伏性结核感染提供有效治疗（这对消除结核病至关重要）的需求促使了本次综述。在本综述中，我们考虑了具有抗结核潜力的羧酰胺衍生物的合成及构效关系研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/49899e382972/IJMC2014-614808.sch.010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/27ee7283375b/IJMC2014-614808.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/8bace946b7bc/IJMC2014-614808.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/41c1fbaab584/IJMC2014-614808.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/84354c2ac01d/IJMC2014-614808.sch.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/43ee4a857656/IJMC2014-614808.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/a49acfe95009/IJMC2014-614808.sch.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/528d38a41dce/IJMC2014-614808.sch.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/c070d758e547/IJMC2014-614808.sch.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/9418f003522c/IJMC2014-614808.sch.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/1fcf4cce5cce/IJMC2014-614808.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/4a1014d4d666/IJMC2014-614808.sch.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/9d75338e2a15/IJMC2014-614808.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/252d6e8d56d8/IJMC2014-614808.sch.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/49899e382972/IJMC2014-614808.sch.010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/27ee7283375b/IJMC2014-614808.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/8bace946b7bc/IJMC2014-614808.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/41c1fbaab584/IJMC2014-614808.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/84354c2ac01d/IJMC2014-614808.sch.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/43ee4a857656/IJMC2014-614808.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/a49acfe95009/IJMC2014-614808.sch.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/528d38a41dce/IJMC2014-614808.sch.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/c070d758e547/IJMC2014-614808.sch.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/9418f003522c/IJMC2014-614808.sch.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/1fcf4cce5cce/IJMC2014-614808.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/4a1014d4d666/IJMC2014-614808.sch.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/9d75338e2a15/IJMC2014-614808.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/252d6e8d56d8/IJMC2014-614808.sch.009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c19d/4295614/49899e382972/IJMC2014-614808.sch.010.jpg

相似文献

1
Synthesis and structural activity relationship study of antitubercular carboxamides.抗结核羧酰胺的合成及其构效关系研究
Int J Med Chem. 2014;2014:614808. doi: 10.1155/2014/614808. Epub 2014 Dec 30.
2
Tuberculosis结核病
3
[Development of antituberculous drugs: current status and future prospects].[抗结核药物的研发：现状与未来前景]
Kekkaku. 2006 Dec;81(12):753-74.
4
API TB Consensus Guidelines 2006: Management of pulmonary tuberculosis, extra-pulmonary tuberculosis and tuberculosis in special situations.《2006年抗结核药物国际共识指南：肺结核、肺外结核及特殊情况结核病的管理》
J Assoc Physicians India. 2006 Mar;54:219-34.
5
[Prospects for development of new antituberculous drugs].[新型抗结核药物的发展前景]
Kekkaku. 2002 Aug;77(8):573-84.
6
Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.N-取代2-氨基噻唑衍生物作为抗结核药物的设计、合成及构效关系研究
Eur J Med Chem. 2014 Jan 24;72:26-34. doi: 10.1016/j.ejmech.2013.11.007. Epub 2013 Nov 13.
7
[Characteristics and treatment outcomes of INH-resistant or RFP-resistant tuberculosis].[耐异烟肼或耐利福平结核病的特征及治疗结果]
Kekkaku. 2003 Oct;78(10):611-7.
8
Benefits of continuous isoniazid preventive therapy may outweigh resistance risks in a declining tuberculosis/HIV coepidemic.在结核病/艾滋病合并感染率不断下降的情况下，异烟肼连续预防性治疗的益处可能超过耐药风险。
AIDS. 2016 Nov 13;30(17):2715-2723. doi: 10.1097/QAD.0000000000001235.
9
Standard short-course chemotherapy for drug-resistant tuberculosis: treatment outcomes in 6 countries.耐多药结核病的标准短程化疗：6个国家的治疗结果
JAMA. 2000 May 17;283(19):2537-45. doi: 10.1001/jama.283.19.2537.
10
Editorial: Current status and perspective on drug targets in tubercle bacilli and drug design of antituberculous agents based on structure-activity relationship.社论：结核杆菌药物靶点的现状与展望以及基于构效关系的抗结核药物设计
Curr Pharm Des. 2014;20(27):4305-6. doi: 10.2174/1381612819666131118203915.

引用本文的文献

1
Construction, petro-collecting/dispersing capacities, antimicrobial activity, and molecular docking study of new cationic surfactant-sulfonamide conjugates.新型阳离子表面活性剂-磺酰胺共轭物的构建、集油/散油能力、抗菌活性及分子对接研究
J Mol Liq. 2021 Jul 15;334:116068. doi: 10.1016/j.molliq.2021.116068. Epub 2021 Apr 8.
2
Novel Leu-Val Based Dipeptide as Antimicrobial and Antimalarial Agents: Synthesis and Molecular Docking.基于亮氨酸-缬氨酸的新型二肽作为抗菌和抗疟药物：合成与分子对接
Front Chem. 2020 Nov 24;8:583926. doi: 10.3389/fchem.2020.583926. eCollection 2020.
3
Biological Activity Evaluation of Some New Benzenesulphonamide Derivatives.

本文引用的文献

1
Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.发现四氢吡唑并嘧啶甲酰胺衍生物作为强效口服活性抗结核药物。
ACS Med Chem Lett. 2013 Apr 1;4(5):451-5. doi: 10.1021/ml400071a. eCollection 2013 May 9.
2
Fueling open-source drug discovery: 177 small-molecule leads against tuberculosis.推动开源药物研发：177 个针对结核病的小分子先导化合物。
ChemMedChem. 2013 Feb;8(2):313-21. doi: 10.1002/cmdc.201200428. Epub 2013 Jan 10.
3
A chemical genetic screen in Mycobacterium tuberculosis identifies carbon-source-dependent growth inhibitors devoid of in vivo efficacy.
一些新型苯磺酰胺衍生物的生物活性评价
Front Chem. 2019 Sep 18;7:634. doi: 10.3389/fchem.2019.00634. eCollection 2019.
结核分枝杆菌的化学遗传学筛选鉴定出无体内疗效的碳源依赖性生长抑制剂。
Nat Commun. 2010 Aug 24;1(5):57. doi: 10.1038/ncomms1060.
4
Synthesis and antimycobacterial evaluation of novel Phthalazin-4-ylacetamides against log- and starved phase cultures.新型苯并二嗪-4-基乙酰胺的合成及对对数期和饥饿期培养物的抗分枝杆菌活性评价。
Chem Biol Drug Des. 2010 Apr;75(4):381-91. doi: 10.1111/j.1747-0285.2010.00947.x. Epub 2010 Feb 8.
5
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.新型抗结核 2,10-二氢-4aH-色烯并[3,2-c]吡啶-3-基衍生物的发现。
Eur J Med Chem. 2010 Jan;45(1):120-3. doi: 10.1016/j.ejmech.2009.09.033. Epub 2009 Sep 20.
6
5-Nitrothiazolylthiosemicarbazones: synthesis and antimycobacterial evaluation against tubercular and non-tubercular mycobacterial species.5-硝基噻唑基硫代氨基脲：针对结核分枝杆菌和非结核分枝杆菌物种的合成及抗分枝杆菌活性评估。
J Enzyme Inhib Med Chem. 2010 Feb;25(1):105-10. doi: 10.3109/14756360903027451.
7
Substituted N-Phenylpyrazine-2-carboxamides: synthesis and antimycobacterial evaluation.取代 N-苯基吡嗪-2-甲酰胺：合成与抗分枝杆菌活性评价。
Molecules. 2009 Oct 20;14(10):4180-9. doi: 10.3390/molecules14104180.
8
Antituberculosis activity of the molecular libraries screening center network library.分子库筛选中心网络库的抗结核活性。
Tuberculosis (Edinb). 2009 Sep;89(5):354-63. doi: 10.1016/j.tube.2009.07.006. Epub 2009 Sep 26.
9
L-proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines.L-脯氨酸催化的简便绿色方法合成[1,4]噻嗪并并评估其抗分枝杆菌活性。
Eur J Med Chem. 2009 Dec;44(12):4978-84. doi: 10.1016/j.ejmech.2009.09.001. Epub 2009 Sep 6.
10
An atom economic synthesis and antitubercular evaluation of novel spiro-cyclohexanones.新型螺环己酮的原子经济性合成及抗结核活性评价
Bioorg Med Chem Lett. 2009 Jul 1;19(13):3461-5. doi: 10.1016/j.bmcl.2009.05.018. Epub 2009 May 9.