Suppr超能文献

一种作为三种寄生虫病潜在治疗药物的呋咱并[3,4-b]哒嗪-阿莫地喹杂合物()。

A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().

作者信息

Mott Bryan T, Cheng Ken Chih-Chien, Guha Rajarshi, Kommer Valerie P, Williams David L, Vermeire Jon J, Cappello Michael, Maloney David J, Rai Ganesha, Jadhav Ajit, Simeonov Anton, Inglese James, Posner Gary H, Thomas Craig J

机构信息

Department of Chemistry, Zanvyl Krieger School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland, 21218, USA ; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland, 20892, USA.

出版信息

Medchemcomm. 2012 Dec;3(12):1505-1511. doi: 10.1039/C2MD20238G.

Abstract

Parasitic diseases continue to have a devastating impact on human populations worldwide. Lack of effective treatments, the high cost of existing ones, and frequent emergence of resistance to these agents provide a strong argument for the development of novel therapies. Here we report the results of a hybrid approach designed to obtain a dual acting molecule that would demonstrate activity against a variety of parasitic targets. The antimalarial drug amodiaquine has been covalently joined with a nitric oxide-releasing furoxan to achieve multiple mechanisms of action. Using in vitro and ex vivo assays, the hybrid molecule shows activity against three parasites - Plasmodium falciparum, Schistosoma mansoni, and Ancylostoma ceylanicum.

摘要

寄生虫病继续对全球人类群体产生毁灭性影响。缺乏有效的治疗方法、现有治疗方法成本高昂以及对这些药物的耐药性频繁出现,都有力地支持了开发新型疗法的必要性。在此,我们报告一种混合方法的结果,该方法旨在获得一种具有双重作用的分子,该分子将对多种寄生虫靶点显示活性。抗疟药物阿莫地喹已与释放一氧化氮的呋咱共价连接,以实现多种作用机制。通过体外和离体试验,该杂交分子对三种寄生虫——恶性疟原虫、曼氏血吸虫和锡兰钩虫显示出活性。

相似文献

本文引用的文献

1
Drug hybridization strategies: before or after lead identification?药物杂交策略:是在先导化合物鉴定之前还是之后?
Expert Opin Drug Discov. 2009 Jun;4(6):605-9. doi: 10.1517/17460440902956636. Epub 2009 May 6.

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