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
Ravindra mishra
, Anoop singh
CLK (casein like kinase), Down syndrome, potential inhibitors
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.
"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", IJSDR - International Journal of Scientific Development and Research (www.IJSDR.org), ISSN:2455-2631, Vol.5, Issue 6, page no.154 - 159, June-2020, Available :https://ijsdr.org/papers/IJSDR2006026.pdf
Volume 5
Issue 6,
June-2020
Pages : 154 - 159
Paper Reg. ID: IJSDR_191918
Published Paper Id: IJSDR2006026
Downloads: 000347204
Research Area: Pharmacy
Country: Datia, madhya pradesh, India
ISSN: 2455-2631 | IMPACT FACTOR: 9.15 Calculated By Google Scholar | ESTD YEAR: 2016
An International Scholarly Open Access Journal, Peer-Reviewed, Refereed Journal Impact Factor 9.15 Calculate by Google Scholar and Semantic Scholar | AI-Powered Research Tool, Multidisciplinary, Monthly, Multilanguage Journal Indexing in All Major Database & Metadata, Citation Generator
Publisher: IJSDR(IJ Publication) Janvi Wave
