INTERNATIONAL JOURNAL OF SCIENTIFIC DEVELOPMENT AND RESEARCH International Peer Reviewed & Refereed Journals, Open Access Journal ISSN Approved Journal No: 2455-2631 | Impact factor: 8.15 | ESTD Year: 2016
open access , Peer-reviewed, and Refereed Journals, Impact factor 8.15
STRUCTURE BASED DRUG DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF (E)-4-(BENZYLIDENEAMINO)-6- PHENYL-3-THIOXO-3,4-DIHYDRO -1,2,4-TRIAZIN-5(2H)-ONE DERIVATIVES AS CLK1A AND DYRK1A INHIBITORS
Authors Name:
Ravindra mishra
, Anoop singh
Unique Id:
IJSDR2006026
Published In:
Volume 5 Issue 6, June-2020
Abstract:
A series of novel -4-(BENZYLIDENEAMINO)-6- PHENYL-3-THIOXO-3,4-DIHYDRO -1,2,4-TRIAZIN-5(2H)-ONE derivatives (3a–3j) has been synthesized and evaluated as potential inhibitors for protein kinases implicated in Alzheimer’s disease. Among all the synthesized compounds, compound 3e (N-(3,4-dimethoxyphenyl)-6,7-dimethoxyquinazolin-4-amine) exhibited the most potent inhibitory activity against CLK1 and GSK-3a/b kinase with IC50 values of 1.5 lM and 3 lM, respectively. Docking studies were performed to elucidate the binding mode of the compounds to the active site of CLK1 and GSK-3b. The results of our study suggest that compound 3e may serve as a valuable template for the design and development of dual inhibitors of CLK1 and GSK-3a/b enzymeswith potential therapeutic application in Alzheimer’s disease.
Keywords:
CLK (casein like kinase), Down syndrome, potential inhibitors
Cite Article:
"STRUCTURE BASED DRUG DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF (E)-4-(BENZYLIDENEAMINO)-6- PHENYL-3-THIOXO-3,4-DIHYDRO -1,2,4-TRIAZIN-5(2H)-ONE DERIVATIVES AS CLK1A AND DYRK1A INHIBITORS", International Journal of Science & Engineering Development Research (www.ijsdr.org), ISSN:2455-2631, Vol.5, Issue 6, page no.154 - 159, June-2020, Available :http://www.ijsdr.org/papers/IJSDR2006026.pdf
Downloads:
000336256
Publication Details:
Published Paper ID: IJSDR2006026
Registration ID:191918
Published In: Volume 5 Issue 6, June-2020
DOI (Digital Object Identifier):
Page No: 154 - 159
Publisher: IJSDR | www.ijsdr.org
ISSN Number: 2455-2631
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