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Molecules 2017, 22(6), 970;

Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents

Basic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, China
Author to whom correspondence should be addressed.
Received: 28 April 2017 / Revised: 6 June 2017 / Accepted: 9 June 2017 / Published: 14 June 2017
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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 511 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. View Full-Text
Keywords: rhodanine; N-arylsulfonylindole; propanoic acid; antibacterial activity rhodanine; N-arylsulfonylindole; propanoic acid; antibacterial activity

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Song, M.-X.; Li, S.-H.; Peng, J.-Y.; Guo, T.-T.; Xu, W.-H.; Xiong, S.-F.; Deng, X.-Q. Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents. Molecules 2017, 22, 970.

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