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首页> 外文期刊>Archiv der Pharmazie >Synthesis and biological evaluation of 2-mercapto-1,3-benzothiazole derivatives with potential antimicrobial activity.
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Synthesis and biological evaluation of 2-mercapto-1,3-benzothiazole derivatives with potential antimicrobial activity.

机译：具有潜在抗菌活性的2-巯基-1,3-苯并噻唑衍生物的合成和生物学评估。

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摘要

The enhancement of bacterial resistance of pathogens to currently available antibiotics constitutes a serious public health threat. So, intensive efforts are underway worldwide to develop new antimicrobial agents. To identify compounds with a potent antimicrobial profile, we designed and synthesized low molecular weight 2-mercaptobenzothiazole derivatives 2a-2l and 3a-3l. Both series were screened for in-vitro antibacterial activity against the representative panel of Gram-positive and Gram-negative bacteria strains. The biological screening identified compounds 2e and 2l as the most active ones showing an interesting antibacterial activity with MIC values of 3.12 microg/mL against Staphylococcus aureus and 25 microg/mL against Escherichia coli, respectively. The replacement of the S-H by the S-Bn moiety resulted in considerable loss of the antibacterial action of the 3a-3l series. The antibiotic action of compounds 2e and 2l was also investigated by testing their activity against some clinical isolates with different antimicrobial resistance profile. Moreover, the involvement of the NorA efflux pump in the antibacterial activity of our molecules was evaluated. Finally, in this paper, we also describe the cytotoxic activity of the most interesting compounds by MTS assay against HeLa and MRC-5 cell lines.
机译：病原体对当前可用抗生素的细菌抵抗力的增强构成了严重的公共卫生威胁。因此，世界范围内正在努力开发新的抗微生物剂。为了鉴定具有有效抗菌特性的化合物，我们设计并合成了低分子量2-巯基苯并噻唑衍生物2a-2l和3a-3l。筛选了两个系列的针对革兰氏阳性和革兰氏阴性细菌菌株的代表性小组的体外抗菌活性。生物学筛选确定化合物2e和2l为最具活性的化合物，它们显示出令人感兴趣的抗菌活性，其对金黄色葡萄球菌的MIC值分别为3.12 microg / mL和对大肠杆菌的MIC值为25 microg / mL。用S-Bn部分取代S-H导致3a-3l系列抗菌作用的明显丧失。还通过测试化合物2e和2l对某些具有不同抗菌素耐药性的临床分离株的活性来研究其抗菌作用。此外，还评估了NorA外排泵对我们分子的抗菌活性的影响。最后，在本文中，我们还通过MTS分析描述了最有趣的化合物对HeLa和MRC-5细胞系的细胞毒活性。

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