New Thiosemicarbazide Derivatives with Multidirectional Biological Action

Molecules. 2024 Mar 29;29(7):1529. doi: 10.3390/molecules29071529.

Abstract

Over the years, several new medicinal substances have been introduced for the treatment of diseases caused by bacteria and parasites. Unfortunately, due to the production of numerous defense mechanisms by microorganisms and parasites, they still pose a serious threat to humanity around the world. Therefore, laboratories all over the world are still working on finding new, effective methods of pharmacotherapy. This research work aimed to synthesize new compounds derived from 3-trifluoromethylbenzoic acid hydrazide and to determine their biological activity. The first stage of the research was to obtain seven new compounds, including six linear compounds and one derivative of 1,2,4-triazole. The PASS software was used to estimate the potential probabilities of biological activity of the newly obtained derivatives. Next, studies were carried out to determine the nematocidal potential of the compounds with the use of nematodes of the genus Rhabditis sp. and antibacterial activity using the ACCT standard strains. To determine the lack of cytotoxicity, tests were performed on two cell lines. Additionally, an antioxidant activity test was performed due to the importance of scavenging free radicals in infections with pathogenic microorganisms. The conducted research proved the anthelmintic and antibacterial potential of the newly obtained compounds. The most effective were two compounds with a 3-chlorophenyl substituent, both linear and cyclic derivatives. They demonstrated higher efficacy than the drugs used in treatment.

Keywords: antibacterial activity; antioxidant activity; cytotoxic effect; nematocidal activity; synthesis; thiosemicarbazides.

MeSH terms

  • Anti-Bacterial Agents* / pharmacology
  • Antinematodal Agents*
  • Cell Line
  • Hydrazines
  • Semicarbazides*

Substances

  • thiosemicarbazide
  • Anti-Bacterial Agents
  • Antinematodal Agents
  • Hydrazines
  • Semicarbazides

Grants and funding

This research was funded by Medical University of Lublin, Poland, grants number DS 15 and DS 43.