Basha, Shaik Jeelan published the artcileNew Flavone-Cyanoacetamide Hybrids with a Combination of Cholinergic, Antioxidant, Modulation of β-Amyloid Aggregation, and Neuroprotection Properties as Innovative Multifunctional Therapeutic Candidates for Alzheimer’s Disease and Unraveling Their Mechanism of Action with Acetylcholinesterase, Synthetic Route of 15029-36-4, the publication is Molecular Pharmaceutics (2018), 15(6), 2206-2223, database is CAplus and MEDLINE.
In line with the modern multi target-directed ligand paradigm of Alzheimer’s disease (AD), a series of nineteen compounds composed of flavone and cyanoacetamide groups have been synthesized and evaluated as multifunctional agents against AD. Biol. evaluation demonstrated that compounds 7j, 7n, 7o, 7r and 7s exhibited excellent inhibitory potency (AChE, IC50 0.271 ± 0.012 to ± 0.075 M) and good selectivity toward acetylcholinesterase, significant antioxidant activity, good modulation effects on self-induced Aβ aggregation, low cytotoxicity and neuroprotection in human neuroblastoma SK-N-SH cells. Further, an inclusive study on the interaction of 7j, 7n, 7o, 7r and 7s with AChE at physiol. pH 7.2 using fluorescence, CD and mol. docking methods suggesting that these derivatives bind strongly to peripheral anionic site of AChE mostly through hydrophobic interactions. Overall, the multifunctional profiles and strong AChE binding affinity highlight these compounds as promising prototypes for further pursuit of innovative multifunctional drugs for AD.
Molecular Pharmaceutics published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, Synthetic Route of 15029-36-4.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics