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Description
Imidazole derivatives are well known for their broad spectrum of biological activities and significant applications in medicinal and agrochemical research, including anticancer, antifungal, antibacterial, anti-inflammatory, and neuroprotective effects.1 In addition to their medicinal importance, acetylcholinesterase (AChE) inhibitors are widely used as active ingredients in insecticidal plant protection products, while butyrylcholinesterase (BuChE) is also known to be inhibited by organophosphate and carbamate pesticides and is frequently used as a biomarker of pesticide exposure. Consequently, the evaluation of both AChE and BuChE inhibition provides valuable insight into the potency, selectivity, and potential safety of newly synthesized compounds in agrochemical research.2 In this work, a series of novel arylamide derivatives of 1H-imidazole-4-carboxylic acid was synthesized using a modified Steglich amidation method with EDC × HCl and DMAP under mild reaction conditions. Structural modifications included the incorporation of aniline and meta- or para-substituted aniline moieties containing electron-donating or electron-withdrawing groups in order to investigate structure–activity relationships. All compounds were characterized by melting point determination, 1H and 13C NMR spectroscopy, and mass spectrometry. The synthesized derivatives evaluated for their inhibitory activity against both AChE and BuChE, in order to obtain a more comprehensive insight into their cholinesterase inhibition profile.
Keywords: acetylcholinesterase, butyrylcholinesterase, imidazole, 1H-imidazole-4-carboxylic acid
References:
1. Al-Ghamdi, HA; Almughem, FA; Alshabibi, MA; Bakr, AA; Alshehri, AA; Aodah, AH; Al Zahrani, NA; Tawfik, EA; Damiati, LA. Synthesis and Biological Evaluation of Novel Imidazole Derivatives as Antimicrobial Agents. Biomolecules. 2024, 14, 1198. https://doi.org/10.3390/BIOM14091198/S1
- Karnaš, M; Rastija, V; Šubarić, D; Molnar, M. Green Synthesis and Acetylcholinesterase Inhibition of Coumarin-1,2,4-Triazole Hybrids. Curr. Org. Chem. 2023, 27, 883–892. https://doi.org/10.2174/1385272827666230817145725