Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Arch Pharm (Weinheim) ; 352(3): e1800247, 2019 Mar.
Article in English | MEDLINE | ID: mdl-30638282

ABSTRACT

Four series of novel compounds based on 4-aminopyridine, glatiramer acetate, pyrone, and coumarin backbones were sufficiently synthesized and identified by spectroscopic methods. CYP enzyme inhibition assays of five predominate human P450 isozymes indicate that all compounds, except for 4-hydrazide pyridine 1c, seem to be less toxic than 4-aminopyridine. Further investigation of the compounds using molecular docking experiments revealed different, the same, or stronger binding modes for most of the synthesized compounds, with both polar and hydrophobic interactions with the 1WDA and 1J95 receptors compared to benzoyl l-arginine amide and 4-aminopyridine, respectively. These results introduce the synthesized compounds as K+ channel blockers that could be considered for in vivo CNS disease studies.


Subject(s)
4-Aminopyridine/chemical synthesis , 4-Aminopyridine/pharmacology , Coumarins/chemical synthesis , Coumarins/pharmacology , Cytochrome P-450 Enzyme System/metabolism , Potassium Channels/metabolism , 4-Aminopyridine/analogs & derivatives , Central Nervous System Diseases/drug therapy , Central Nervous System Diseases/enzymology , Coumarins/chemistry , Drug Discovery , Humans , Molecular Docking Simulation , Molecular Structure , Protein Binding
SELECTION OF CITATIONS
SEARCH DETAIL
...