The catalytic potential of pyridine-2-carboxlic acid has been evaluated for efficient, green and solvent free synthesis of 2,4,5-trisubstituted imidazole derivatives. The compounds were synthesized by condensation reaction of substituted aromatic aldehydes, benzil and ammonium acetate ( 3a-3m ) in one pot in a good to excellent yield (74-96 %). These compounds were evaluated against acetylcholinesterase (AChE) enzyme activity to explore their potential against Alzheimer’s disease. Among this series of compounds 3m bearing one ethoxy and a hydroxyl group on the phenyl ring on 2,4,5-trisubstituted imidazoles proved potent AChE inhibitor (102.56±0.14). Structure-activity relationship (SAR) of these compounds was developed. Molecular dockings were carried out for the inhibitors 3m , 3e , 3k , 3c , 3a , 3d , 3j , and 3f in order to further investigate the binding mechanism. The inhibitor molecule was molecularly docked with acetylcholinesterase to further study its binding mechanism. The amino group of the inhibitor 3m forms an H bond with the oxygen atom of the residue (i.e., THR121), and has a bond length of 3.051 Å.© 2020 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
June 4, 2020
September 3, 2020
- ACC 2020The American College of Cardiology decided to cancel ACC.20/WCC due to COVID-19, which was scheduled to take place March 28-30 in Chicago. However, ACC.20/WCC Virtual Meeting continues to release cutting edge science and practice changing updates for cardiovascular professionals on demand and free through June 2020.
- ENDO: 2020ENDO 2020 Annual Conference has been canceled due to COVID-19. Here are highlights of emerging data that has still been released. Keep an eye out for ENDO Online 2020, which will take place from June 8 to 22.
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