| Title : Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach - Ceschi_2016_Eur.J.Med.Chem_121_758 |
| Author(s) : Ceschi MA , da Costa JS , Lopes JP , Camara VS , Campo LF , Borges AC , Goncalves CA , de Souza DF , Konrath EL , Karl AL , Guedes IA , Dardenne LE |
| Ref : Eur Journal of Medicinal Chemistry , 121 :758 , 2016 |
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Abstract :
Tianeptine was linked to various 9-aminoalkylamino-1,2,3,4-tetrahydroacridines using EDC.HCl/HOBt to afford a series of tacrine-tianeptine hybrids. The hybrids were tested for their ability to inhibit AChE and BuChE and IC50 values in the nanomolar concentration scale were obtained. AChE molecular modeling studies of these hybrids indicated that tacrine moiety interacts in the bottom of the gorge with the catalytic active site (CAS) while tianeptine binds to peripheral anionic site (PAS). Furthermore, the compounds 2g and 2e were able to reduce the in vitro basal secretion of S100B, suggesting its therapeutic action in some cases or stages of Alzheimer's disease. |
| PubMedSearch : Ceschi_2016_Eur.J.Med.Chem_121_758 |
| PubMedID: 27392529 |
Ceschi MA, da Costa JS, Lopes JP, Camara VS, Campo LF, Borges AC, Goncalves CA, de Souza DF, Konrath EL, Karl AL, Guedes IA, Dardenne LE (2016)
Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach
Eur Journal of Medicinal Chemistry
121 :758
Ceschi MA, da Costa JS, Lopes JP, Camara VS, Campo LF, Borges AC, Goncalves CA, de Souza DF, Konrath EL, Karl AL, Guedes IA, Dardenne LE (2016)
Eur Journal of Medicinal Chemistry
121 :758