Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents
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, urgen...
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| Format: | Article |
| Language: | English |
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MDPI AG
2017-06-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/22/6/970 |
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| author | Ming-Xia Song Song-Hui Li Jiao-Yang Peng Ting-Ting Guo Wen-Hui Xu Shao-Feng Xiong Xian-Qing Deng |
| author_facet | Ming-Xia Song Song-Hui Li Jiao-Yang Peng Ting-Ting Guo Wen-Hui Xu Shao-Feng Xiong Xian-Qing Deng |
| author_sort | Ming-Xia Song |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-13T22:15:52Z |
| format | Article |
| id | doaj.art-bf21b51b44e342fbb7b10dbca96ff3ce |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-13T22:15:52Z |
| publishDate | 2017-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-bf21b51b44e342fbb7b10dbca96ff3ce2022-12-21T23:29:33ZengMDPI AGMolecules1420-30492017-06-0122697010.3390/molecules22060970molecules22060970Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial AgentsMing-Xia Song0Song-Hui Li1Jiao-Yang Peng2Ting-Ting Guo3Wen-Hui Xu4Shao-Feng Xiong5Xian-Qing Deng6Basic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaBasic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaBasic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaBasic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaBasic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaBasic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaBasic Medical and Pharmacy College, Jinggangshan University, Ji’an 343009, Jiangxi, ChinaDue 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.http://www.mdpi.com/1420-3049/22/6/970rhodanineN-arylsulfonylindolepropanoic acidantibacterial activity |
| spellingShingle | Ming-Xia Song Song-Hui Li Jiao-Yang Peng Ting-Ting Guo Wen-Hui Xu Shao-Feng Xiong Xian-Qing Deng Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents Molecules rhodanine N-arylsulfonylindole propanoic acid antibacterial activity |
| title | Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents |
| title_full | Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents |
| title_fullStr | Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents |
| title_full_unstemmed | Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents |
| title_short | Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents |
| title_sort | synthesis and bioactivity evaluation of n arylsulfonylindole analogs bearing a rhodanine moiety as antibacterial agents |
| topic | rhodanine N-arylsulfonylindole propanoic acid antibacterial activity |
| url | http://www.mdpi.com/1420-3049/22/6/970 |
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