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Synthesis, antibacterial and antiproliferative potential of some new 1-pyridinecarbonyl-4-substituted thiosemicarbazide derivatives.


ABSTRACT: In this study, the antibacterial, cytotoxic and antiproliferative activities of novel thiosemicarbazide derivatives were assessed. Our results demonstrated that some of the novel compounds possess good antibacterial properties against Staphylococcus epidermidis, Streptococcus mutans and Streptococcussanguinis and are only slightly cytotoxic; thus, they exhibit an excellent therapeutic index, which is higher than that of ethacridine lactate. Moreover, our data showed that compounds 2 and 4 have an antiproliferative activity against human breast adenocarcinoma and human hepatocellular carcinoma cell lines. We expect that the novel thiosemicarbazide derivatives can be used as agents for treatment of dental caries and also for chemotherapy support.

SUBMITTER: Pitucha M 

PROVIDER: S-EPMC4958397 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature

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Synthesis, antibacterial and antiproliferative potential of some new 1-pyridinecarbonyl-4-substituted thiosemicarbazide derivatives.

Pitucha Monika M   Woś Maciej M   Miazga-Karska Malgorzata M   Klimek Katarzyna K   Mirosław Barbara B   Pachuta-Stec Anna A   Gładysz Agata A   Ginalska Grazyna G  

Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents 20160601


In this study, the antibacterial, cytotoxic and antiproliferative activities of novel thiosemicarbazide derivatives were assessed. Our results demonstrated that some of the novel compounds possess good antibacterial properties against <i>Staphylococcus epidermidis</i>, <i>Streptococcus mutans</i> and <i>Streptococcus</i><i>sanguinis</i> and are only slightly cytotoxic; thus, they exhibit an excellent therapeutic index, which is higher than that of ethacridine lactate. Moreover, our data showed t  ...[more]

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