| Title : Novel Tadalafil Derivatives Ameliorates Scopolamine-Induced Cognitive Impairment in Mice via Inhibition of Acetylcholinesterase (AChE) and Phosphodiesterase 5 (PDE5) - Ni_2018_ACS.Chem.Neurosci_9_1625 |
| Author(s) : Ni W , Wang H , Li X , Zheng X , Wang M , Zhang J , Gong Q , Ling D , Mao F , Zhang H , Li J |
| Ref : ACS Chem Neurosci , 9 :1625 , 2018 |
| Abstract : On the basis of the drug-repositioning and redeveloping strategy, first-generation dual-target inhibitors of acetylcholinesterase (AChE) and phosphodiesterase 5 (PDE5) have been recently reported as a potentially novel therapeutic method for the treatment of Alzheimer's disease (AD), and the lead compound 2 has proven this method was feasible in AD mouse models. In this study, our work focused on exploring alternative novel tadalafil derivatives (3a-s). Among the 19 analogues, compound 3c exhibited good selective dual-target AChE/PDE5 inhibition and good blood-brain barrier (BBB) permeability. Moreover, its citrate (3c.Cit) possessed improved water solubility and good effects against scopolamine-induced cognitive impairment with inhibition of cortical AChE activities and enhancement of cAMP response element-binding protein (CREB) phosphorylation ex vivo. |
| ESTHER : Ni_2018_ACS.Chem.Neurosci_9_1625 |
| PubMedSearch : Ni_2018_ACS.Chem.Neurosci_9_1625 |
| PubMedID: 29616790 |
Ni W, Wang H, Li X, Zheng X, Wang M, Zhang J, Gong Q, Ling D, Mao F, Zhang H, Li J (2018)
Novel Tadalafil Derivatives Ameliorates Scopolamine-Induced Cognitive Impairment in Mice via Inhibition of Acetylcholinesterase (AChE) and Phosphodiesterase 5 (PDE5)
ACS Chem Neurosci
9 :1625
Ni W, Wang H, Li X, Zheng X, Wang M, Zhang J, Gong Q, Ling D, Mao F, Zhang H, Li J (2018)
ACS Chem Neurosci
9 :1625