Novel Derivatives of Nicotinic Acid: Synthesis, Crystal Structure, Antimicrobial Activity and Cytotoxicity
Izabela Czyżewska1, Liliana Mazur2, Anna Biernasiuk3
1Chair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, Lublin, Poland.
Abstract:
The overuse of antibiotics is one of the reasons which has led to the development of drug-resistant bacteria, which is a huge challenge for modern medicine. As well as the incidences of cancer, which are increasing every year, currently known cytostatics do not provide satisfactory therapeutic effects with many side effects. Bearing in mind these problems of modern medicine, we have synthesized new acylhydrazones with potential antibacterial and anticancer activities. The compounds were created as a result of condensation of commercially available nicotinic acid hydrazide with appropriate aldehydes. Additionally, some of them were obtained using mechanochemistry. The chemical structure of the obtained compounds was confirmed by spectral methods IR, 1H NMR and 13C NMR, and the crystal structure of selected compounds was determined by single-crystal X-ray diffraction analysis. Phase purity tests were performed for each compound. The tested compounds had very significant activity against Gram-positive bacteria and slightly worse activity against fungi from the genus Candida. The least antibacterial activity of obtained acylhydrazones was shown against Gram-negative bacterial strains. In addition to these, the compounds described did not have a toxic effect on normal cell lines.
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