Thioethers as Potential Antibacterial Agents Against Methicillin-resistant Staphylococcus Aureus (mrsa)
Year: 2026
Type: preprint
Abstract: The emergence and rapid spread of methicillin-resistant Staphylococcus aureus (MRSA) have created an urgent need for new antibacterial agents capable of overcoming established resistance mechanisms. Among the diverse sulfur-containing scaffolds, thioethers have attracted increasing attention because of their structural versatility and ability to modulate antibacterial activity through incorporation into different pharmacophores. This review provides a comprehensive overview of synthetic, semisynthetic, and natural or natural-product-derived thioether compounds evaluated against MRSA, with emphasis on their structural features, structure-activity relationships (SAR), antibacterial potency, and mechanisms of action. The major classes discussed include aminoglycoside-derived thioether amphiphiles, membrane-active small-molecule thioethers, quinazolinone and quinoline thioether scaffolds, pleuromutilin thioether derivatives, SecA-targeting thioethers, chalcone and oxazolidinone derivatives, FtsZ-targeting thioethers, anti-virulence and antibiofilm agents, antimicrobial peptidomimetics, and natural-product-derived thioether compounds. The studies demonstrate that sulfur-containing motifs can contribute to anti-MRSA activity through membrane disruption, inhibition of bacterial protein synthesis and targeting of essential non-ribosomal proteins. The available SAR evidence highlights the scaffold-dependent nature of thioether activity and supports their continued exploration as versatile structural motifs for the development of new therapeutic strategies against drug-resistant MRSA.
Source: ChemRxiv
Authors: Aditya G Lavekar, Radha Ahuja, Deepti Gairola
Language: English
Subfield: Infectious Diseases
Field: Medicine
Domain: Health Sciences
Open Access status: green
OpenAlex ID: W7211897970