| Title : Design, Synthesis, and biological evaluation of pyrazolo-benzothiazole derivatives as a potential therapeutic agent for the treatment of Alzheimers disease - Kumar_2022_Med.Chem.Res_31_1931 |
| Author(s) : Kumar H , Goyal A , Kumar N , Garg P |
| Ref : Med Chem Res , 31 :1931 , 2022 |
|
Abstract :
Alzheimers disease (AD) is a neurodegenerative age-related brain disease which diminishes learning and memory. Two main cholinesterases (ChEs), first acetylcholinesterase (AChE) and second one butyrylcholinesterase (BChE) are the major targets to treat this disease. In the current study, six novel pyrazolo-benzothiazole analogues were systematically planned, synthesized, and biological tested for their ChEs activities, antioxidant, enzyme kinetic, self-induced A modulation, PAMPA-BBB, and docking and molecular simulation study. Among all derivatives, compound 4a bearing 3,4-dimethoxypyrazolo-benzothiazole was the potential inhibitor of AChE (IC50 = 8.69 0.42 M), A modulator and good antioxidant property. Docking studies also clearly revealed that compound 4a fit fully into the active sites of hAChE. |
| PubMedSearch : Kumar_2022_Med.Chem.Res_31_1931 |
| PubMedID: |
Kumar H, Goyal A, Kumar N, Garg P (2022)
Design, Synthesis, and biological evaluation of pyrazolo-benzothiazole derivatives as a potential therapeutic agent for the treatment of Alzheimers disease
Med Chem Res
31 :1931
Kumar H, Goyal A, Kumar N, Garg P (2022)
Med Chem Res
31 :1931