| Title : Synthesis and activity of miconazole derivatives as dual BChE\/IDO1 inhibitors for the treatment of Alzheimer's disease - Lu_2021_Future.Med.Chem_13_1105 |
| Author(s) : Lu X , Liu Y , Qin N , Yang H , Qiao Y , Jiang X , Chen Y , Feng F , Liu W , Zhou Y , Sun H |
| Ref : Future Med Chem , 13 :1105 , 2021 |
|
Abstract :
Background: Alzheimer's disease is a multifactorial neurological disorder seen in elderly people. Loss of cholinergic transmission and unbalanced tryptophan metabolism kynurenine pathway have been demonstrated in neuropsychiatric diseases. Methods & results: Among the two series of synthesized compounds, compounds 5c and 5h were identified as effective dual BChE/IDO1 inhibitors, with well-balanced micromolar activity. Compounds 5c and 5h exhibited promising ability to ameliorate behavioral impairment by Morris water maze. The safety of miconazole analogs was also validated by PC12 and SH-SY5Y cell lines. Conclusion: These results highlight the ability of 5c and 5h to treat Alzheimer's disease. |
| PubMedSearch : Lu_2021_Future.Med.Chem_13_1105 |
| PubMedID: 33960203 |
Lu X, Liu Y, Qin N, Yang H, Qiao Y, Jiang X, Chen Y, Feng F, Liu W, Zhou Y, Sun H (2021)
Synthesis and activity of miconazole derivatives as dual BChE\/IDO1 inhibitors for the treatment of Alzheimer's disease
Future Med Chem
13 :1105
Lu X, Liu Y, Qin N, Yang H, Qiao Y, Jiang X, Chen Y, Feng F, Liu W, Zhou Y, Sun H (2021)
Future Med Chem
13 :1105