4553-27-9Relevant articles and documents
Synthesis of 2-(2-oxo-2H-chromen-4-yl)acetamides as potent acetylcholinesterase inhibitors and molecular insights into binding interactions
Kara, Jiraporn,Suwanhom, Paptawan,Wattanapiromsakul, Chatchai,Nualnoi, Teerapat,Puripattanavong, Jindaporn,Khongkow, Pasarat,Lee, Vannajan Sanghiran,Gaurav, Anand,Lomlim, Luelak
, (2019/07/08)
Sixteen novel coumarin-based compounds are reported as potent acetylcholinesterase (AChE) inhibitors. The most active compound in this series, 5a (IC50 0.04 ± 0.01 μM), noncompetitively inhibited AChE with a higher potency than tacrine and gala
RADIOLABELED COMPOUNDS AND METHODS THEREOF
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Page/Page column 125; 127-128, (2011/12/14)
The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.
A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers
Roufos, Ioannis,Hays, Sheryl,Schwarz, Roy D.
, p. 1514 - 1520 (2007/10/03)
A structure-activity relationship study of a series of novel Na+ channel blockers, structurally related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]- α-phenylbenzeneacetamide (1, PD85639) is described. The diphenylacetic acid portion of the molecule was left unchanged throughout the study, while structural features in the amine portion and the amide alkyl linkage of the molecule were modified. The compounds were tested for inhibition of veratridine-stimulated Na+ influx in CHO cells expressing type IIA Na+ channels. Several derivatives show a trend toward more potent Na+ channel blockade activity with increasing lipophilicity of the amine portion of the molecule. The presence of a phenyl ring near the amine increases inhibitory potency. A three-carbon spacer between the amide and amine is optimal, and a secondary amide linkage is preferred.