SYNTHESIS, CHARACTERIZATION & IN-VITRO ACTIVITY OF NEW SERIES OF COUMARIN SUBSTITUTED MERCAPTO-1, 3, 4-OXADIAZOLE DERIVATIVES AS GSK-3β INHIBITORS

Main Author: Purohit S.S.*, Kulkarni V.H., Joshi S.D.
Format: Article Journal
Terbitan: , 2020
Subjects:
3
Online Access: https://zenodo.org/record/4247133
Daftar Isi:
  • A new series of 2, 5-disubstituted-mercapto-1,3,4-oxadiazole derivatives were synthesized in good yield by reacting different coumarin hydrazide with carbon disulfide & further reacting with various aryl halides. The reactions were monitored by TLC & all derivatives were purified by recrystallization using suitable solvents. The synthesized derivatives were characterized by IR,1H-NMR, Mass spectral data. Further these derivatives were studied for their in-vitro GSK-3β inhibitory activity by using Kinase-Glo Plus luminescence kinase assay & percentage inhibitions were calculated. The standard compound used was CHIR-99021. Some of the derivatives have shown significant in-vitro activity.