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Bioorg Chem ; 71: 170-180, 2017 04.
Article in English | MEDLINE | ID: mdl-28259376

ABSTRACT

An efficient and environmentally benign simple fusion reaction of 3-chloro-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine (1a) or 3-chloro-6-(3,5-dimethyl-4-nitro-1H-pyrazol-1-yl)pyridazine (2a) with different aliphatic/aromatic amines have produced a series of novel pyrazolylpyridazine amines (4a-4c &5a-5m). All compounds exhibited moderate in vitro yeast α-glucosidase inhibition except m-chloro derivative 5g, which was found potent inhibitor of this enzyme with IC50 value of 19.27±0.005µM. The molecular docking further helped in understanding the structure activity relationship of these compounds including 5g.


Subject(s)
Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Pyridazines/chemistry , Pyridazines/pharmacology , Saccharomyces cerevisiae/enzymology , alpha-Glucosidases/metabolism , Amination , Glycoside Hydrolase Inhibitors/chemical synthesis , Green Chemistry Technology/methods , Molecular Docking Simulation , Pyridazines/chemical synthesis , Saccharomyces cerevisiae/chemistry , Saccharomyces cerevisiae/drug effects , Structure-Activity Relationship , alpha-Glucosidases/chemistry
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