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Bioorg Chem ; 79: 64-71, 2018 09.
Article in English | MEDLINE | ID: mdl-29723743

ABSTRACT

A regio and stereo- selective synthesis of hitherto unexplored hybrid heterocyclic system comprising spiropyrrolidine, indolizino[6,7-b]indole units in good to excellent yields, has been developed via three component 1,3-dipolar cycloaddition and concomitant trifluoroacetic acid catalyzed Pictet-Spengler cyclization with paraformaldehyde. The newly synthesized compounds were evaluated for their in vitro acetylcholinesterase (AChE) and butylcholinesterase (BChE) enzyme inhibitory activities. Most of the synthesized compounds showed good inhibitory activity, among them, compounds 4d and 4g displayed highest potency against AChE (IC50 1.88 and 1.98 µM), and BChE (IC50 18.32 and 10.21 µM) enzyme, respectively than the standard drug, galanthamine. Molecular modeling simulation was investigated for the most active compounds 4d and 4g on AChE and BChE enzymes to disclose the binding and orientation of these molecules into active site of respective receptors.


Subject(s)
Cholinesterase Inhibitors/chemistry , Indoles/chemistry , Indolizines/chemistry , Pyrrolidines/chemistry , Spiro Compounds/chemistry , Acetylcholinesterase/chemistry , Animals , Butyrylcholinesterase/chemistry , Catalytic Domain , Cholinesterase Inhibitors/chemical synthesis , Electrophorus , Horses , Hydrogen Bonding , Hydrophobic and Hydrophilic Interactions , Indoles/chemical synthesis , Indolizines/chemical synthesis , Molecular Docking Simulation , Pyrrolidines/chemical synthesis , Spiro Compounds/chemical synthesis
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