Department of Basic Sciences, Faculty of Science, Erzurum Technical University, 25050, Erzurum, Turkey.
J Antibiot (Tokyo). 2021 Apr;74(4):233-243. doi: 10.1038/s41429-020-00399-7. Epub 2021 Jan 14.
Addressed herein a series of thioureas starting from various amines and nicotinic acid have been synthesized. Notably, thiourea based scaffolds are increasingly employed in medicinal chemistry owing to their tunable physicochemical and structural properties. As well-known from the literature, the pyridine ring contains various biological properties, especially antimicrobial activity. Therefore, we performed the synthesis of biologically important thiourea derivatives containing pyridine ring. The structures of the synthesized compounds were characterized by H NMR, C NMR and FT-IR. In the second part of the study, newly synthesized compounds were also tested in order to demonstrate their antimicrobial and antioxidant properties. All compounds exhibited moderate activity against all tested bacteria known to cause nosocomial infections, which have acquired resistance to many antibiotics, as compared to the standard antibiotics and also strong antioxidant properties. Therefore, they can be evaluated as possible seeds of agents in the treatment of bacterial infections and many health problems related to aging such as cancer, and neurodegenerative diseases.
本文合成了一系列由不同胺和烟酸衍生而来的硫脲类化合物。值得注意的是，硫脲类支架由于其可调节的物理化学和结构性质，在药物化学中越来越多地被应用。正如文献中所熟知的，吡啶环具有多种生物特性，特别是抗菌活性。因此，我们合成了含有吡啶环的具有生物重要性的硫脲衍生物。合成化合物的结构通过 H NMR、C NMR 和 FT-IR 进行了表征。在研究的第二部分，还测试了新合成的化合物，以证明它们的抗菌和抗氧化特性。与标准抗生素相比，所有化合物对所有已知引起医院感染且对许多抗生素产生耐药性的测试细菌均表现出中等活性，并且具有很强的抗氧化特性。因此，它们可以被评估为治疗细菌感染和与衰老相关的许多健康问题（如癌症和神经退行性疾病）的潜在药物的候选物。
