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Université de Caen Basse-Normandie, Centre d'Etudes et de Recherche sur le Médicament de Normandie (UPRES EA 4258 – FR CNRS 3038 INC3M) UFR des Sciences Pharmaceutiques, Bd Becquerel, 14032 Caen cedex, France
; Fax: +33 2 31 56 68 03
; Tel: +33 2 31 56 68 03
Med. Chem. Commun., 2012,3, 627-634
04 Mar 2012,
20 Mar 2012
First published online
23 Mar 2012
The synthesis of novel pyrrolothienopyrazines has been achieved with the aim to bring together in a sole compound both AChE inhibitory effect and 5-HT4R agonist activity. These Multi-Target Directed Ligands might theoretically alleviate the cognitive deficit in Alzheimer disease by restoring the cholinergic activity and by promoting the non-amyloidogenic formation of sAPPα which seems detrimental to the amyloid aggregation. Some of the synthesized compounds bear for the first time these dual activities and compound 15b appears particularly potent towards both AChE and 5-HT4R targets with IC50 and Ki in nanomolar levels. Although these MTDL behave as 5-HT4R antagonists rather than agonists, these results appear hopeful concerning the design of further MTDL with therapeutic interest in AD treatment.
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