New Thiosemicarbazide Derivatives with Multidirectional Biological Action

Author:

Lasek Patryk1ORCID,Kosikowska Urszula2ORCID,Kołodziej Przemysław3ORCID,Kubiak-Tomaszewska Grażyna4,Krzyżanowska Natalia3ORCID,Szostek Tomasz4,Struga Marta4ORCID,Feldo Marcin5,Bogucka-Kocka Anna3ORCID,Wujec Monika6ORCID

Affiliation:

1. Doctoral School, Medical University of Lublin, Chodzki 7, 20-093 Lublin, Poland

2. Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University, 20-093 Lublin, Poland

3. Department of Biology and Genetics, Faculty of Pharmacy, Medical University of Lublin, 4A Chodzki Street, 20-093 Lublin, Poland

4. Department of Biochemistry, Medical University of Warsaw, 02-097 Warszawa, Poland

5. Department of Vascular Surgery, Medical University of Lublin, Staszica 11 St., 20-081 Lublin, Poland

6. Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodzki Street, 20-093 Lublin, Poland

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.

Funder

Medical University of Lublin, Poland

Publisher

MDPI AG

Reference81 articles.

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