期刊论文详细信息
Molecules
Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents
Wen-Hui Xu1  Shao-Feng Xiong1  Xian-Qing Deng1  Ming-Xia Song1  Ting-Ting Guo1  Song-Hui Li1  Jiao-Yang Peng1 
[1] Basic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, China;
关键词: rhodanine;    N-arylsulfonylindole;    propanoic acid;    antibacterial activity;   
DOI  :  10.3390/molecules22060970
来源: DOAJ
【 摘 要 】

Due to the rapidly growing bacterial resistance to antibiotics and the scarcity of novel agents under development, bacterial infections are still a pressing global problem, making new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, urgently needed. In this paper, seven series of N-arylsulfonylindole analogs 5–11 bearing rhodanine moieties were synthesized, characterized, and evaluated for antibacterial activity. According to the in vitro antimicrobial results, half of the synthesized compounds showed potent inhibition against four Gram-positive bacteria, with MIC values in the range of 0.5–8 µg/mL. For multidrug-resistant strains, compounds 6a and 6c were the most potent, with MIC values of 0.5 µg/mL, having comparable activity to gatifloxacin, moxiflocaxin and norfloxacin and being 128-fold more potent than oxacillin (MIC = 64 µg/mL) and 64-fold more active than penicillin (MIC = 32 µg/mL) against Staphylococcus aureus ATCC 43300.

【 授权许可】

Unknown   

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