ArticleNaunyn-Schmiedeberg's archives of pharmacology2026
Novel 1,2,3-triazole-thiophene hybrids: synthesis, anti-MRSA/MSSA activity, antioxidant potential, and acetylcholinesterase ınhibition supported by molecular docking.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
The discovery of single-molecule therapeutics capable of simultaneously addressing antibiotic resistance and neurodegeneration represents a critical unmet need in modern medicinal chemistry. Herein, I report the rational design and efficient one-pot synthesis of a novel class of 1,2,3-triazole-thiophene hybrids (2a-2e) as dual-target bioactive agents. This streamlined synthetic approach afforded the target compounds in good yields, with substituent effects playing a decisive role in reaction efficiency. Biological evaluation revealed a pronounced enhancement in antibacterial activity, with several compounds exhibiting potent efficacy against both methicillin-susceptible and methicillin-resistant Staphylococcus aureus (MRSA). In particular, compounds 2d and 2e demonstrated remarkable potency, achieving minimum inhibitory concentration (MIC) values as low as 2 µg/mL against MRSA. Structure-activity relationship analysis identified para-halogen substitution as a key determinant of antibacterial performance. Beyond their antibacterial effects, the hybrids displayed significant acetylcholinesterase (AChE) inhibitory activity, with compounds 2c (IC
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