Thiadiazole and Thiazole Derivatives as Potential Antimicrobial Agents

Abstract

Background: This review summarizes data on heterocyclic systems with thiadiazole and thiazole fragments in molecules as promising antimicrobial agents Introduction: Thiadiazole and thiazole backbones are the most favored and well-known heterocycles, a common and essential feature of various drugs. These scaffolds occupy a central position and are the main structural components of numerous drugs with a wide spectrum of action. These include antimicrobial, antituberculous, anti-inflammatory, analgesic, antiepileptic, antiviral, and anticancer agents. Method: The research is based on bibliosemantic and analytical methods using bibliographic and abstract databases, as well as databases of chemical compounds. Result: This review reports on thiadiazole and thiazole derivatives, which have important pharmacological properties. We are reviewing the structural modifications of various thiadiazole and thiazole derivatives, more specifically, the antimicrobial activity reported over the last years, as we have taken this as our main research area. 80 compounds were illustrated, and various derivatives containing hydrazone bridged thiazole and pyrrole rings, 2-pyridine and 4-pyridine substituted thiazole derivatives, compounds containing di-, tri- and tetrathiazole moieties, Spiro-substituted 4-thiazolidinone-imidazoline-pyridines were analyzed. Derivatives of 5-heteroarylidene-2,4-thiazolidinediones, fluoroquinolone-thiadiazole hybrids, and others. Conclusion: 1,3,4-thiadiazoles and thiazoles are valuable resource for researchers engaged in rational drug design and development in this area.

Exploring the potential of bis(thiazol-5-yl)phenylmethane derivatives as novel candidates against genetically defined multidrug-resistant Staphylococcus aureus

“…Thiazole inherent chemical properties, such as reactive and electron-rich structure, lend themselves well to various substitutions, allowing the generation of diverse derivatives with enhanced bioactivity. Moreover, thiazole derivatives, often has moderate lipophilicity and the potential for hydrogen bonding, contribute to favorable pharmacokinetic profiles [16,17]. Thiazole derivatives have displayed efficacy against a various pathogenic organism, including WHO priority listed pathogens [16,17].…”

“…Moreover, thiazole derivatives, often has moderate lipophilicity and the potential for hydrogen bonding, contribute to favorable pharmacokinetic profiles [16,17]. Thiazole derivatives have displayed efficacy against a various pathogenic organism, including WHO priority listed pathogens [16,17]. Depending on the structural substitutions, these compounds often target essential microbial processes such as DNA synthesis, protein translation, and direct and indirect cell wall biosynthesis [16,18].…”

“…The sulfur atom within the thiazole ring can coordinate with metal ions crucial for microbial enzyme activity, adding another layer to their antimicrobial mechanism [18,32]. The thiazole nucleus containing compound shows favorable biological properties with the ability to interact with diverse microbial targets including cell wall synthesis pathway, thus making thiazole-based compounds as a promising scaffold for the development of novel and effective antimicrobial agents for further pre-clinical evaluation against multidrug-resistant S. aureus or other Gram-positive pathogens [11,14,17,32].…”