Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland.
Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Faculty of Pharmacy, Department of Inorganic and Analytical Chemistry, 85-094 Bydgoszcz, Poland.
Curr Med Chem. 2019;26(4):664-693. doi: 10.2174/0929867325666180228164656.
Antibiotic resistance acquired by various bacterial fungal and viral pathogens poses therapeutic problems of increasing severity. Among the infections that are very difficult to treat, biofilm-associated cases are one of the most hazardous. Complex structure of a biofilm and unique physiology of the biofilm cells contribute to their extremely high resistance to environmental conditions, antimicrobial agents and the mechanisms of host immune response. Therefore, the biofilm formation, especially by multidrugresistant pathogens, is a serious medical problem, playing a pivotal role in the development of chronic and recurrent infections. These factors create a limitation for using traditional chemiotherapeutics and contribute to a request for development of new approaches for treatment of infectious diseases. Therefore, early reports on antimicrobial activity of several complexes of metal ions, bearing thiosemicarbazide or thiosemicarbazones as the ligands, gave a boost to worldwide search for new, more efficient compounds of this class, to be used as alternatives to commonly known drugs. In general, depending on the presence of other heteroatoms, these ligands may function in a di-, tri- or tetradentate forms (e.g., of N,S,-, N,N,S-, N,N,N,S-, N,N,S,S-, or N,S,O-type), which impose different coordination geometries to the resultant complexes. In the first part of this review, we describe the ways of synthesis and the structures of the ligands based on the thiosemicarbazone motif, while the second part deals with the antimicrobial activity of their complexes with selected metal ions.
各种细菌、真菌和病毒病原体获得的抗生素耐药性带来了越来越严重的治疗问题。在非常难以治疗的感染中,生物膜相关的病例是最危险的之一。生物膜的复杂结构和生物膜细胞的独特生理学导致它们对环境条件、抗菌剂和宿主免疫反应机制具有极高的抵抗力。因此,生物膜的形成,特别是由多药耐药病原体引起的生物膜的形成,是一个严重的医学问题,在慢性和复发性感染的发展中起着关键作用。这些因素限制了传统化学疗法的使用,并促使人们寻求新的方法来治疗传染病。因此,关于几种金属离子配合物的抗菌活性的早期报告,这些配合物以硫代氨基甲酰肼或硫代氨基甲酰腙作为配体,推动了全世界对新的、更有效的这类化合物的搜索,以替代常用的已知药物。一般来说,根据存在其他杂原子,这些配体可以以二齿、三齿或四齿(例如,N,S-、N,N,S-、N,N,N,S-、N,N,S,S-或 N,S,O-型)的形式发挥作用,这会给所得配合物带来不同的配位几何形状。在这篇综述的第一部分,我们描述了基于硫代氨基甲酰腙基序的配体的合成方法和结构,而第二部分则涉及它们与选定金属离子的配合物的抗菌活性。