Open AccessDOCKING STUDIES AND SYNTHESIS OF NOVEL 4- THIAZOLIDINONE DERIVATIVES BEARING 1, 3, 4- OXADIAZOLE MOIETY AS SIRT-3 ACTIVATORS TARGETING PARKINSON’S DISEASE
Author(s) -
Gomathy Sandhya Subramanian,
Farhath Sherin,
Naina Merin Joy,
Ashish D Wadhwan,
Gowramma Byran,
A Shanish Antony
Publication year - 2022
Publication title -
rasayan journal of chemistry/rasayan journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.281
H-Index - 22
eISSN - 0976-0083
pISSN - 0974-1496
DOI - 10.31788/rjc.2022.1516628
Subject(s) - oxadiazole , cytotoxicity , mtt assay , moiety , in silico , chemistry , docking (animal) , in vitro , sirt3 , histone deacetylase , sirtuin , biochemistry , cancer research , stereochemistry , microbiology and biotechnology , biology , histone , gene , acetylation , medicine , organic chemistry , nursing
Seven protein families known as class III histone deacetylase for their characteristic features have been reported in mammals. Sirtuin3 (SIRT3) has gained considerable attention among the sirtuin members for its role in neurodegenerative disease. A new series of 4-thiazolidinones fused 1, 3, 4-oxadiazole derivatives have been designed in silico by using Schrodinger software. Molecules showing high affinity with the target protein (4JSR) were selected for the synthesis and analytical methods were used to determine the structures. The synthesized compounds III (a-h) were taken for in vitro cytotoxicity studies by MTT assay technique using SHSY5Y neuroblastoma cell lines. The synthesized compounds III (a-h) were taken for in vitro cytotoxicity studies by MTT assay technique using SHSY5Y neuroblastoma cell lines. Gene expression study was then performed on SIRT-3 gene by reverse transcriptase PCR method. Compound III b and III g were effective with IC50 values of 126.70 and 157.42 respectively and were found to possess good expression on the SIRT-3 gene.