| Literature DB >> 27392529 |
Marco Antonio Ceschi1, Jessie Sobieski da Costa2, João Paulo Bizarro Lopes2, Viktor Saraiva Câmara2, Leandra Franciscato Campo2, Antonio César de Amorim Borges2, Carlos Alberto Saraiva Gonçalves3, Daniela Fraga de Souza3, Eduardo Luis Konrath4, Ana Luiza Martins Karl5, Isabella Alvim Guedes5, Laurent Emmanuel Dardenne6.
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.Entities:
Keywords: AChE; BuChE; Coupling reaction; Molecular modeling; S100B secretion; Tacrine; Tianeptine
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Year: 2016 PMID： 27392529 DOI： 10.1016/j.ejmech.2016.06.025
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514