Chemical Biology & Drug Design 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 C12H10O4S, Name: 2-Cyano-N-ethylacetamide.
Shaik, Jeelan Basha published the artcileSynthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer’s Disease, Name: 2-Cyano-N-ethylacetamide, the publication is Chemical Biology & Drug Design (2016), 88(1), 43-53, database is CAplus and MEDLINE.
Alzheimer’s disease onset and progression are associated with the dysregulation of multiple and complex physiol. processes, and a successful therapeutic approach should therefore address more than one target. In line with this modern paradigm, a series of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene analogs (4a-q) were synthesized and evaluated for their multitarget-directed activity on acetylcholinesterase, butyrylcholinesterase (BuChE), 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical, and amyloid-β peptide (Aβ) specific targets for Alzheimer’s disease therapy. Most of the synthesized compounds showed remarkable acetylcholinesterase inhibitory activities in low nM concentrations and good ABTS radical scavenging activity, however, no evidence of BuChE inhibitory activity. Among them, 3-bromobenzylamide derivative N-(3-bromobenzyl)-8-imino-2-oxo-2H,8H-pyrano [2,3-f]chromene-9-carboxamide (4m) exhibited the best acetylcholinesterase inhibitory activity with IC50 value of 13±1.4 nM which is 51-fold superior to galantamine, a reference drug. Kinetic and mol. docking studies indicated (4m) as mixed-type inhibitor, binding simultaneously to catalytic active and peripheral anionic sites of acetylcholinesterase. Five compounds N-cyclohexyl-8-imino-2-oxo-2H,8H-pyrano[2,3-f] chromene-9-carboxamide (4e), 8-imino-9-(morpholine-4-carbonyl)-2H,8H-pyrano [2,3-f]chromen-2-one (4f), N-benzyl-8-imino-2-oxo-2H,8H-pyrano[2,3-f] chromene-9-carboxamide (4g), 8-imino-N-(1-(4-methoxyphenyl)ethyl)-2-oxo-2H,8H- pyrano[2,3-f]chromene-9-carboxamide (4j), and N-(2,4-dimethoxybenzyl)-8-imino-2-oxo-2H,8H- pyrano[2,3-f]chromene-9-carboxamide (4k) have shown 1.4- to 2.5-fold of higher antioxidant activities than trolox. Interestingly, the most active compound (4m) demonstrated dosage-dependent acceleration of Aβ1-42 aggregation, which may reduce toxicity of oligomers. Overall, these results lead to discovery of fused tricyclic coumarins as promising dual binding site inhibitors of acetylcholinesterase and afford multifunctional compounds with potential impact for further pharmacol. development in Alzheimer’s therapy.
Chemical Biology & Drug Design 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 C12H10O4S, Name: 2-Cyano-N-ethylacetamide.
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https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics