Loesche_2016_Eur.J.Med.Chem_125_430

Reference

Title : Repurposing N,N'-bis-(arylamidino)-1,4-piperazinedicarboxamidines: An unexpected class of potent inhibitors of cholinesterases - Loesche_2016_Eur.J.Med.Chem_125_430
Author(s) : Loesche A , Wiese J , Sommerwerk S , Simon V , Brandt W , Csuk R
Ref : Eur Journal of Medicinal Chemistry , 125 :430 , 2016
Abstract :

Drug repurposing (=drug repositioning) is an effective way to cut costs for the development of new therapeutics and to reduce the time-to-market time-span. Following this concept a small library of compounds was screened for their ability to act as inhibitors of acetyl- and butyrylcholinesterase. Picloxydine, an established antiseptic, was shown to be an inhibitor for both enzymes. Systematic variation of the aryl substituents led to analogs possessing almost the same good properties as gold standard galantamine hydrobromide.

PubMedSearch : Loesche_2016_Eur.J.Med.Chem_125_430
PubMedID: 27689726

Related information

Citations formats

Loesche A, Wiese J, Sommerwerk S, Simon V, Brandt W, Csuk R (2016)
Repurposing N,N'-bis-(arylamidino)-1,4-piperazinedicarboxamidines: An unexpected class of potent inhibitors of cholinesterases
Eur Journal of Medicinal Chemistry 125 :430

Loesche A, Wiese J, Sommerwerk S, Simon V, Brandt W, Csuk R (2016)
Eur Journal of Medicinal Chemistry 125 :430