Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents.
Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents.
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含绕丹宁结构的N-芳基磺酰吲哚类似物抗菌剂的合成及生物活性评价
DOI：
10.3390/molecules22060970
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发表时间：
2017-06-14
期刊：
影响因子：
--
通讯作者：
Deng XQ
中科院分区：
文献类型：
--
作者：
Song MX;Li SH;Peng JY;Guo TT;Xu WH;Xiong SF;Deng XQ
由于细菌对抗生素的耐药性迅速增长，以及正在开发的新型药物的稀缺性，细菌感染仍然是一个紧迫的全球性问题，因此迫切需要单独使用和与传统抗生素联合使用的新型抗菌剂。本文合成了7个含绕丹宁结构的N-芳基磺酰基吲哚类化合物5-11，并对其进行了结构表征和抗菌活性评价。根据体外抗菌结果，一半的合成化合物对四种革兰氏阳性菌表现出有效的抑制作用，MIC值在0.5-8 µg/mL范围内。对于多药耐药菌株，化合物6a和6c是最有效的，MIC值为0.5 μg/mL，具有与加替沙星、氟沙星和诺氟沙星相当的活性，并且对金黄色葡萄球菌ATCC 43300的有效性是苯唑西林（MIC = 64 μg/mL）的128倍，活性是青霉素（MIC = 32 μg/mL）的64倍。
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.
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DOI：
10.3390/molecules21081070
发表时间：
2016-08-16
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Vera G;Lagos CF;Almendras S;Hebel D;Flores F;Valle-Corvalán G;Pessoa-Mahana CD;Mella-Raipán J;Montecinos R;Recabarren-Gajardo G
通讯作者：
Recabarren-Gajardo G
影响因子：
5.6
作者：
Tay SB;Yew WS
通讯作者：
Yew WS
影响因子：
6.7
作者：
Jin, Xin;Zheng, Chang-Ji;Piao, Hu-Ri
通讯作者：
Piao, Hu-Ri
影响因子：
6.7
作者：
Song, Ming-Xia;Zheng, Chang-Ji;Piao, Hu-Ri
通讯作者：
Piao, Hu-Ri
影响因子：
5.2
作者：
Livermore, David M.
通讯作者：
Livermore, David M.