β-苯乙胺基喹唑啉-4-胺作为细胞色素氧化酶的有效抑制剂的合成及其构效关系
Syntheses and Structure-Activity Relationships of -Phenethyl-Quinazolin-4-yl-Amines as Potent Inhibitors of Cytochrome Oxidase in .
作者信息
Hopfner Sarah M, Lee Bei Shi, Kalia Nitin P, Miller Marvin J, Pethe Kevin, Moraski Garrett C
机构信息
Department of Chemistry and Biochemistry, Montana State University, 103 Chemistry and Biochemistry Building, Bozeman, Montana, MT 59717, USA.
School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore.
出版信息
Appl Sci (Basel). 2021 Oct;11(19). doi: 10.3390/app11199092. Epub 2021 Sep 29.
The development of cytochrome oxidase (cyt-) inhibitors are needed for comprehensive termination of energy production in (Mtb) to treat tuberculosis infections. Herein, we report on the structure-activity-relationships (SAR) of 22 new -phenethyl-quinazolin-4-yl-amines that target cyt-. Our focused set of compounds was synthesized and screened against three mycobacterial strains: BCG, H37Rv and the clinical isolate N0145 with and without the cytochrome inhibitor Q203 in an ATP depletion assay. Two compounds, and , were more active against all three strains than the naturally derived cyt- inhibitor aurachin D.
为了全面终止结核分枝杆菌（Mtb）的能量产生以治疗结核病感染，需要开发细胞色素氧化酶（cyt-）抑制剂。在此，我们报告了22种靶向cyt-的新型β-苯乙基喹唑啉-4-基胺的构效关系（SAR）。我们合成了一组重点化合物，并在ATP消耗试验中针对三种分枝杆菌菌株进行筛选：卡介苗（BCG）、H37Rv和临床分离株N0145，试验中添加和不添加细胞色素氧化酶抑制剂Q203。在针对所有三种菌株的活性方面，两种化合物，即[具体化合物1]和[具体化合物2]，比天然衍生的cyt-抑制剂金精D更具活性。
Zotero 插件