Verheijen_2009_Bioorg.Med.Chem.Lett_19_3243

Reference

Title : Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition - Verheijen_2009_Bioorg.Med.Chem.Lett_19_3243
Author(s) : Verheijen JC , Wiig KA , Du S , Connors SL , Martin AN , Ferreira JP , Slepnev VI , Kochendorfer U
Ref : Bioorganic & Medicinal Chemistry Lett , 19 :3243 , 2009
Abstract :

Conjugation of the phenol derived from rivastigmine with amphetamines gave access to novel carbamate cholinesterase inhibitors. All compounds possessed increased affinity and selectivity for AChE compared to rivastigmine and were orally bioavailable. Compound 4a, incorporating d-amphetamine, caused significant inhibition of cholinesterase in vivo at doses that were well tolerated. Release of amphetamine from 4a was demonstrated following in vitro and in vivo inhibition of cholinesterase. Compound 4a was also effective in alleviating scopolamine induced amnesia in a rat passive avoidance model.

PubMedSearch : Verheijen_2009_Bioorg.Med.Chem.Lett_19_3243
PubMedID: 19423342

Related information

Inhibitor CHEMBL1784957
Substrate CHEMBL1784957    CHEMBL1784957

Citations formats

Verheijen JC, Wiig KA, Du S, Connors SL, Martin AN, Ferreira JP, Slepnev VI, Kochendorfer U (2009)
Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition
Bioorganic & Medicinal Chemistry Lett 19 :3243

Verheijen JC, Wiig KA, Du S, Connors SL, Martin AN, Ferreira JP, Slepnev VI, Kochendorfer U (2009)
Bioorganic & Medicinal Chemistry Lett 19 :3243