Kheruka SC

References (1)

Title : Design and development of novel p-aminobenzoic acid derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease - Shrivastava_2018_Bioorg.Chem_82_211
Author(s) : Shrivastava SK , Sinha SK , Srivastava P , Tripathi PN , Sharma P , Tripathi MK , Tripathi A , Choubey PK , Waiker DK , Aggarwal LM , Dixit M , Kheruka SC , Gambhir S , Shankar S , Srivastava RK
Ref : Bioorg Chem , 82 :211 , 2018
Abstract : Based on the quantitative structure-activity relationship (QSAR), some novel p-aminobenzoic acid derivatives as promising cholinesterase enzyme inhibitors were designed, synthesized, characterized and evaluated to enhance learning and memory. The in vitro enzyme kinetic study of the synthesized compounds revealed the type of inhibition on the respective acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vivo studies of the synthesized compounds exhibited significant reversal of cognitive deficits in the animal models of amnesia as compared to standard drug donepezil. Further, the ex vivo studies in the specific brain regions like the hippocampus, hypothalamus, and prefrontal cortex regions also exhibited AChE inhibition comparable to standard donepezil. The in silico molecular docking and dynamics simulations studies of the most potent compound 22 revealed the consensual interactions at the active site pocket of the AChE.
ESTHER : Shrivastava_2018_Bioorg.Chem_82_211
PubMedSearch : Shrivastava_2018_Bioorg.Chem_82_211
PubMedID: 30326403