6个″-十胺磺酰乙酰胺功能化的阿米卡星和卡那霉素两亲性衍生物的合成及其抗菌活性

IF 1 4区化学 Q4 CHEMISTRY, MULTIDISCIPLINARY

Australian Journal of Chemistry Pub Date : 2023-11-13 DOI:10.1071/ch23154

Dylan C. Farr, Lendl Tan, Juanelle Furness, I. Darren Grice, Nicholas P. West, Todd A. Houston

{"title":"6个″-十胺磺酰乙酰胺功能化的阿米卡星和卡那霉素两亲性衍生物的合成及其抗菌活性","authors":"Dylan C. Farr, Lendl Tan, Juanelle Furness, I. Darren Grice, Nicholas P. West, Todd A. Houston","doi":"10.1071/ch23154","DOIUrl":null,"url":null,"abstract":"Aminoglycoside antibiotics represent the first class of successful drugs in the treatment of tuberculosis; however, mycobacteria and other bacterial species possess several drug resistance mechanisms to inactivate these natural products. In the past 15 years, a variety of amphiphilic aminoglycosides have been shown to have improved activity against infectious microorganisms and to subvert resistance mechanisms. Here, we report on four novel synthetic compounds derived from two existing potent antitubercular compounds and describe their activity against both Mycobacterium tuberculosis and Staphylococcus aureus. It was found that a decanesulfonylacetamide-based conjugate of amikacin displayed promising preliminary antitubercular activities, warranting further investigation to assess the therapeutic potential of these unique antimicrobials.","PeriodicalId":8575,"journal":{"name":"Australian Journal of Chemistry","volume":null,"pages":null},"PeriodicalIF":1.0000,"publicationDate":"2023-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and antibacterial activity of 6″-decanesulfonylacetamide-functionalised amphiphilic derivatives of amikacin and kanamycin\",\"authors\":\"Dylan C. Farr, Lendl Tan, Juanelle Furness, I. Darren Grice, Nicholas P. West, Todd A. Houston\",\"doi\":\"10.1071/ch23154\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Aminoglycoside antibiotics represent the first class of successful drugs in the treatment of tuberculosis; however, mycobacteria and other bacterial species possess several drug resistance mechanisms to inactivate these natural products. In the past 15 years, a variety of amphiphilic aminoglycosides have been shown to have improved activity against infectious microorganisms and to subvert resistance mechanisms. Here, we report on four novel synthetic compounds derived from two existing potent antitubercular compounds and describe their activity against both Mycobacterium tuberculosis and Staphylococcus aureus. It was found that a decanesulfonylacetamide-based conjugate of amikacin displayed promising preliminary antitubercular activities, warranting further investigation to assess the therapeutic potential of these unique antimicrobials.\",\"PeriodicalId\":8575,\"journal\":{\"name\":\"Australian Journal of Chemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.0000,\"publicationDate\":\"2023-11-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Australian Journal of Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1071/ch23154\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Australian Journal of Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1071/ch23154","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}

引用次数: 0

摘要

氨基糖苷类抗生素是治疗结核病成功的第一类药物;然而，分枝杆菌和其他细菌种类具有几种耐药机制来灭活这些天然产物。在过去的15年中，各种两亲性氨基糖苷已被证明具有提高抗感染性微生物的活性和破坏耐药机制。在这里，我们报道了从两种现有的有效抗结核化合物中衍生出的四种新的合成化合物，并描述了它们对结核分枝杆菌和金黄色葡萄球菌的活性。研究发现，以十烷磺酰乙酰胺为基础的阿米卡星缀合物显示出有希望的初步抗结核活性，需要进一步研究以评估这些独特抗菌剂的治疗潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文本刊更多论文

Synthesis and antibacterial activity of 6″-decanesulfonylacetamide-functionalised amphiphilic derivatives of amikacin and kanamycin

Aminoglycoside antibiotics represent the first class of successful drugs in the treatment of tuberculosis; however, mycobacteria and other bacterial species possess several drug resistance mechanisms to inactivate these natural products. In the past 15 years, a variety of amphiphilic aminoglycosides have been shown to have improved activity against infectious microorganisms and to subvert resistance mechanisms. Here, we report on four novel synthetic compounds derived from two existing potent antitubercular compounds and describe their activity against both Mycobacterium tuberculosis and Staphylococcus aureus. It was found that a decanesulfonylacetamide-based conjugate of amikacin displayed promising preliminary antitubercular activities, warranting further investigation to assess the therapeutic potential of these unique antimicrobials.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Australian Journal of Chemistry 化学-化学综合

CiteScore

2.50

自引率

0.00%

发文量

审稿时长

1.3 months

期刊介绍： Australian Journal of Chemistry - an International Journal for Chemical Science publishes research papers from all fields of chemical science. Papers that are multidisciplinary or address new or emerging areas of chemistry are particularly encouraged. Thus, the scope is dynamic. It includes (but is not limited to) synthesis, structure, new materials, macromolecules and polymers, supramolecular chemistry, analytical and environmental chemistry, natural products, biological and medicinal chemistry, nanotechnology, and surface chemistry. Australian Journal of Chemistry is published with the endorsement of the Commonwealth Scientific and Industrial Research Organisation (CSIRO) and the Australian Academy of Science.