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

Monika Pitucha,Agata Gładysz,Barbara Mirosław,Katarzyna Klimek,Malgorzata Miazga-Karska,Grazyna Ginalska,Anna Pachuta-Stec,Maciej Woś

doi:10.1007/s00044-016-1599-6

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.Electronic supplementary materialThe online version of this article (doi:10.1007/s00044-016-1599-6) contains supplementary material, which is available to authorized users.

Highlights

For many years, new drugs of an interesting structure, unknown molecular target, low toxicity and a high therapeutic index have been looked for
We reported the synthesis and antibacterial activity of new compounds with pyridinecarbonyl group connected to the thiosemicarbazide system
It should be noted that two thiosemicarbazide derivatives, i.e., 2 and 4, exhibited good or moderate inhibition of all the most common caries-associated Gram-positive and Gram-negative bacterial strains

Summary

Introduction

New drugs of an interesting structure, unknown molecular target, low toxicity and a high therapeutic index have been looked for. Our data showed that compounds 2 and 4 have an antiproliferative activity against human breast adenocarcinoma and human hepatocellular carcinoma cell lines. The in vitro activity of the newly synthesized compounds against other tested bacterial strains was found to be lower compared to the controls (Cefepime, CLX and ethacridine lactate).

Results

Conclusion