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Biphenyl-3-oxo-1,2,4-triazine Linked Piperazine Derivatives as Potential Cholinesterase Inhibitors With Anti-Oxidant Property to Improve the Learning and Memory

Biphenyl-3-oxo-1,2,4-triazine Linked Piperazine Derivatives as Potential Cholinesterase Inhibitors With Anti-Oxidant Property to Improve the Learning and Memory

Prabhash Nath Tripathi, Pavan Srivastava, Piyoosh Sharma, Manish Kumar Tripathi, Ankit Seth, Avanish Tripathi, Sachchida Nand Rai, Surya Pratap Singh, Sushant K Shrivastava

Bioorg Chem. 2019 Apr;85:82-96.

PMID: 30605887

Abstract:

A series of novel piperazine tethered biphenyl-3-oxo-1,2,4-triazine derivatives were designed, and synthesized. Amongst the synthesized analogs, compound 6g showed significant non-competitive inhibitory potential against acetylcholinesterase (AChE, IC50; 0.2 ± 0.01 μM) compared to standard donepezil (AChE, IC50: 0.1 ± 0.002 μM). Compound 6g also exhibited significant displacement of propidium iodide from the peripheral anionic site (PAS) of AChE (22.22 ± 1.11%) and showed good CNS permeability in PAMPA-BBB assay (Pe(exp), 6.93 ± 0.46). The in vivo behavioral studies of compound 6g indicated significant improvement in cognitive dysfunctions against scopolamine-induced amnesia mouse models. Further, ex vivo studies showed a significant AChE inhibition and reversal of the scopolamine-induced oxidative stress by compound 6g. Moreover, molecular docking and dynamics simulations of compound 6g showed a consensual binding affinity and active site interactions with the PAS and active catalytic site (CAS) residues of AChE.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP25535164-B	Propidium Iodide - CAS 25535-16-4		25535-16-4	Price

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