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Design, Synthesis, and Antibacterial Activity of Long-Chain Alkyl-Substituted DemethyloxyAaptamine Derivatives

文献类型：期刊论文

作者Liu, Yingqiu2; Wu, Wei4,5; Xue, Haitao3; Wang, Shu-Ping3; Xu, Jing3; Zhang, Tao1,6,7; Lin, Hou-Wen2,3,4,5; Liao, Hongze3
刊名JOURNAL OF NATURAL PRODUCTS
出版日期2025-09-26
卷号88期号:9页码:2097-2106
ISSN号0163-3864
DOI10.1021/acs.jnatprod.5c00571
英文摘要Demethyloxyaaptamine, isolated from the marine sponge Aaptos aaptos, features a 1H-benzo[de][1,6]naphthyridine core and exhibits potent antibacterial activity. To systematically investigate its underexplored antibacterial properties and facilitate structural optimization, we constructed a focused library of 28 C-3 alkylamino-substituted derivatives of demethyloxyaaptamine via regioselective functionalization. In vitro evaluation against Staphylococcus aureus revealed that several derivatives possess minimum inhibitory concentrations (MICs) superior to vancomycin. Structure-activity relationship analysis (SAR) demonstrated that the incorporation of moderately hydrophobic alkylamino groups at the C-3 position markedly improved antimicrobial efficacy. Mechanistic investigations demonstrated that these compounds inhibit bacterial growth by targeting bacterial membrane. Together, these findings validate demethyloxyaaptamine as a privileged scaffold for targeting drug-resistant Gram-positive pathogens and deliver critical SAR insights to guide the design of next-generation antibiotics.
WOS关键词AAPTAMINE DERIVATIVES ; METHICILLIN RESISTANCE ; STAPHYLOCOCCUS-AUREUS ; MECHANISMS ; ALKALOIDS
资助项目National Natural Science Foundation of China
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001574270000001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/321486]  
专题国家级研究中心_原创新药研究全国重点实验室
通讯作者Zhang, Tao; Lin, Hou-Wen; Liao, Hongze
作者单位1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
2.Shanghai Ocean Univ, Sch Food, Shanghai 201306, Peoples R China
3.Shanghai Jiao Tong Univ, Sch Med, Ren Ji Hosp, Dept Pharm,Coll Clin Pharm,State Key Lab Microbial, Shanghai 200127, Peoples R China
4.Shanghai Jiao Tong Univ, Integrated Innovat Ctr Marine Drugs, Shanghai 200240, Peoples R China
5.Marine Biomed Sci & Technol Innovat Platform Linga, Shanghai 201306, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Chem Biol, State Key Lab Drug Res, Shanghai 201203, Peoples R China
7.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Yingqiu,Wu, Wei,Xue, Haitao,et al. Design, Synthesis, and Antibacterial Activity of Long-Chain Alkyl-Substituted DemethyloxyAaptamine Derivatives[J]. JOURNAL OF NATURAL PRODUCTS,2025,88(9):2097-2106.
APA Liu, Yingqiu.,Wu, Wei.,Xue, Haitao.,Wang, Shu-Ping.,Xu, Jing.,...&Liao, Hongze.(2025).Design, Synthesis, and Antibacterial Activity of Long-Chain Alkyl-Substituted DemethyloxyAaptamine Derivatives.JOURNAL OF NATURAL PRODUCTS,88(9),2097-2106.
MLA Liu, Yingqiu,et al."Design, Synthesis, and Antibacterial Activity of Long-Chain Alkyl-Substituted DemethyloxyAaptamine Derivatives".JOURNAL OF NATURAL PRODUCTS 88.9(2025):2097-2106.

入库方式： OAI收割

来源：上海药物研究所

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