Gleyton L.S. Sousa, Douglas C.A. Pinto, Isadora M.G. Andrade, Gustavo S.G. de Carvalho, Fernando C. da Silva
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引用次数: 0
Abstract
Antimicrobial resistance (AMR) has emerged as one of the foremost public health threats of the 21st century. The progressive decline in the efficacy of conventional antibiotics, combined with a scarcity of new drug classes approved in recent decades, has created a critical and alarming scenario. In this context, new biological, chemical, and artificial intelligence tools have played a fundamental role in supporting the discovery of compounds aimed at improving safety, efficacy, and broad-spectrum activity, addressing both AMR and the high costs associated with drug development. Recent data from the World Health Organization (WHO) highlight a list of priority pathogens intended to guide efforts in the search for new therapeutic options. Most compounds currently in preclinical and clinical development are small molecules with direct mechanisms of action. Within this landscape, the search for new molecular scaffolds has focused especially on derivatives of natural compounds and synthetic heterocyclic structures. Among these, derivatives containing the 1,3-thiazole core have stood out due to their synthetic versatility and ability to interact with various bacterial molecular targets. This review provides a comprehensive overview of different classes of thiazole derivatives with demonstrated activity against multidrug-resistant bacterial strains. Their mechanisms of action, relevant chemical, and pharmacological properties, as well as methodological approaches applied to the discovery of these bioactive compounds are discussed highlighting their potential in the development of new therapeutic alternatives to combat bacterial resistance.
期刊介绍:
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.