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1.
ACS Comb Sci ; 17(6): 341-7, 2015 Jun 08.
Article in English | MEDLINE | ID: mdl-25946638

ABSTRACT

Magnetic Fe(OH)3@Fe3O4 nanoparticles were successfully prepared and characterized. This magnetic nanocomposite was employed as an efficient, reusable, and environmentally benign heterogeneous catalyst for the direct amidation of alcohols with amine hydrochloride salts. Several derivatives of primary, secondary and tertiary amides were synthesized in moderate to good yields in the presence of this catalytic system. The catalyst was successfully recycled and reused up to six times without significant loss of its catalytic activity.


Subject(s)
Alcohols/chemistry , Amines/chemistry , Ferric Compounds/chemistry , Amides/chemistry , Catalysis , Indicators and Reagents , Magnetics , Microscopy, Electron, Scanning , Nanoparticles , Oxidation-Reduction , X-Ray Diffraction
2.
Bioorg Chem ; 41-42: 22-7, 2012.
Article in English | MEDLINE | ID: mdl-22341898

ABSTRACT

A novel method has been developed for the synthesis of 1-ureidophosphonates through a three components condensation of aldehyde with amine and diethylphosphite in the presence of sulfanilic acid as catalyst followed by subsequent reaction of the product with isocyanate. This method is easy, rapid, and good yielding. The anticholinesterase (AChE) activities (inhibition potency through IC(50)) of newly synthesized 1-ureidophosphonates were also investigated. The activities of the synthesized compounds toward the enzyme AChE were determined and compared in terms of their molecular structures and it was found, through molecular docking simulations, that the most potent derivative (compound 3i) inhibited the enzyme through binding to the peripheral anionic site (PAS) and not to its acylation site (A site).


Subject(s)
Acetylcholinesterase/chemistry , Cholinesterase Inhibitors/chemical synthesis , Organophosphonates/chemical synthesis , Acetylcholinesterase/metabolism , Aldehydes/chemistry , Amines/chemistry , Binding Sites , Cholinesterase Inhibitors/pharmacology , Computer Simulation , Humans , Models, Molecular , Neurodegenerative Diseases/drug therapy , Neurodegenerative Diseases/enzymology , Organophosphonates/pharmacology , Phosphites/chemistry , Protein Binding , Structure-Activity Relationship , Sulfanilic Acids/chemistry
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