Paper Report for: 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 A, Wiese J, Sommerwerk S, Simon V, Brandt W, Csuk R Ref: Eur Journal of Medicinal Chemistry, 125:430, 2016 : PubMed
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.
        
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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 Chemistry125: 430-434
Loesche A, Wiese J, Sommerwerk S, Simon V, Brandt W, Csuk R (2016) Eur Journal of Medicinal Chemistry125: 430-434