4487-04-1Relevant articles and documents
Development of phthalimide-donepezil hybrids as potent multitargetdirected ligands for the treatment of alzheimer’s disease
Yu, Lintao,Shi, Jian,Cheng, Xinfeng,Wang, Keren,Liu, Shuang,Liu, Wenmin,Sang, Zhipei
, p. 1155 - 1163 (2020/09/15)
Background: Due to the complex etiology of AD, multi-target-directed ligands (MTDLs), combining two or more distinct pharmacological moieties, have been developed in both symptomatic and disease-modifying efficiencies and are considered as an effective way for the treatment of AD. Methods: To test their biological activities, including AChE/BChE inhibitory activity and MAOA/MAO-B inhibitory activity. In addition, molecular modeling studies were performed to afford insight into the binding mode. Results and Discussions: The results displayed that compound 4c showed the best AChE inhibitory activity with an IC50 value of 4.2 μM, which was supported by the kinetic study and docking study. Compound 4c was also a selective MAO-B inhibitor (IC50 = 8.2 μM). Moreover, compound 4c could cross the blood-brain barrier in vitro. Conclusion: Compound 4c deserved to further study as a potential multifunctional agent for the treatment of Alzheimer’s disease.
RADIOLABELED COMPOUNDS AND METHODS THEREOF
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Page/Page column 112; 115-116, (2011/12/14)
The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.