4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity

Luigi Scipione; Daniela De Vita; Alessandra Musella; Lisa Flammini; Simona Bertoni; Elisabetta Barocelli

doi:10.1016/j.bmcl.2007.10.077

4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity

Bioorg Med Chem Lett. 2008 Jan 1;18(1):309-12. doi: 10.1016/j.bmcl.2007.10.077. Epub 2007 Nov 19.

Authors

Luigi Scipione¹, Daniela De Vita, Alessandra Musella, Lisa Flammini, Simona Bertoni, Elisabetta Barocelli

Affiliation

¹ Dipartimento di Studi di chimica e tecnologia delle sostanze biologicamente attive, Sapienza Università di Roma, Piazzale Aldo Moro, 5, 00185 Roma, Italia. luigi.scipione@uniroma1.it

PMID: 18023348
DOI: 10.1016/j.bmcl.2007.10.077

Abstract

Several carbamate derivatives of 4-aminopyridine were synthesized and their anticholinesterase activity was evaluated. Compound 4d showed the highest inhibitory effect blocking non-competitively acetylcholinesterase and competitively butyrylcholinesterase. Furthermore, carbamate 4d was able to revert the amnesic effects of scopolamine in the passive avoidance test in rats.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

4-Aminopyridine / analogs & derivatives*
4-Aminopyridine / chemical synthesis
4-Aminopyridine / pharmacology
Amnesia / chemically induced
Amnesia / drug therapy
Animals
Avoidance Learning / drug effects
Behavior, Animal / drug effects
Carbamates / chemical synthesis
Carbamates / chemistry
Carbamates / pharmacology
Cholinesterase Inhibitors / chemistry*
Cholinesterase Inhibitors / pharmacology*
Kinetics
Rats
Scopolamine / pharmacology

Substances

Carbamates
Cholinesterase Inhibitors
4-Aminopyridine
Scopolamine