Activity Profiling of Nitro-Substituted Di(Hetero)Aryl 1,3,4- and 1,2,4-Oxadiazoles: Antimicrobial, Cholinesterase Inhibition and Antioxidant Potential.

ABSTRACT: Oxadiazole derivatives represent a promising scaffold for drug discovery, offering therapeutic potential, notably against neurodegenerative diseases and microbial infections. Based on molecular hybridisation approach utilising bioactive oxadiazoles, pyridine-, quinoline- and nitrophenyl-based compounds, we designed novel 1,3,4- and 1,2,4-oxadiazole derivatives containing nitro group(s), evaluated their enzyme inhibition, antimicrobial, and antioxidant properties, and analysed their structure-activity relationships (SAR). Comprehensive activity assessments of them and their synthetic precursors revealed robust inhibitory activity against acetylcholinesterase with IC₅₀ values as low as 1.47 µM and butyrylcholinesterase (IC₅₀ ≥ 45.09 μM), outperforming rivastigmine in se

SUBMITTER: Sikorova E 

PROVIDER: S-EPMC12820407 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature