Staśkiewicz Agnieszka, Ledwoń Patrycja, Rovero Paolo, Papini Anna Maria, Latajka Rafal
Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Science and Technology, Wroclaw, Poland.
Interdepartmental Research Unit of Peptide and Protein Chemistry and Biology, Department of Chemistry "Ugo Schiff", University of Florence, Firenze, Italy.
Front Chem. 2021 May 20;9:674705. doi: 10.3389/fchem.2021.674705. eCollection 2021.
Peptidomimetics play a fundamental role in drug design due to their preferential properties regarding natural peptides. In particular, compounds possessing nitrogen-containing heterocycles have been intensively studied in recent years. The triazolyl moiety incorporation decreases the molecule susceptibility to enzymatic degradation, reduction, hydrolysis, and oxidation. In fact, peptides containing triazole rings are a typical example of peptidomimetics. They have all the advantages over classic peptides. Both efficient synthetic methods and biological activity make these systems an interesting and promising object of research. Peptide triazole derivatives display a diversity of biological properties and can be obtained via numerous synthetic strategies. In this review, we have highlighted the importance of the triazole-modified peptidomimetics in the field of drug design. We present an overview on new achievements in triazolyl-containing peptidomimetics synthesis and their biological activity as inhibitors of enzymes or against cancer, viruses, bacteria, or fungi. The relevance of above-mentioned compounds was confirmed by their comparison with unmodified peptides.
由于拟肽相对于天然肽具有独特的性质,因此在药物设计中发挥着重要作用。特别是,含氮杂环化合物近年来受到了广泛研究。引入三唑基部分可降低分子对酶降解、还原、水解和氧化的敏感性。事实上,含三唑环的肽是拟肽的典型例子。它们比经典肽具有所有优势。高效的合成方法和生物活性使这些体系成为一个有趣且有前景的研究对象。肽三唑衍生物具有多种生物学特性,可通过多种合成策略获得。在本综述中,我们强调了三唑修饰的拟肽在药物设计领域的重要性。我们概述了含三唑基拟肽合成的新进展及其作为酶抑制剂或抗癌、抗病毒、抗菌或抗真菌剂的生物活性。通过与未修饰肽的比较,证实了上述化合物的相关性。