TY  - JOUR
AU  - Fiorino, Ferdinando
AU  - Eiden, Martin
AU  - Giese, Armin
AU  - Severino, Beatrice
AU  - Esposito, Antonella
AU  - Groschup, Martin H
AU  - Perissutti, Elisa
AU  - Magli, Elisa
AU  - Incisivo, Giuseppina Maria
AU  - Ciano, Antonio
AU  - Frecentese, Francesco
AU  - Kretzschmar, Hans A
AU  - Wagner, Jens
AU  - Santagada, Vincenzo
AU  - Caliendo, Giuseppe
TI  - Synthesis of benzamide derivatives and their evaluation as antiprion agents.
JO  - Bioorganic & medicinal chemistry
VL  - 20
IS  - 16
SN  - 0968-0896
CY  - Amsterdam [u.a.]
PB  - Elsevier
M1  - DZNE-2020-07560
SP  - 5001-5011
PY  - 2012
AB  - A new set of 5-(2-(pyrrolidin-1-yl)acetamido)-N-butyl-2-(substituted)benzamide and 5-(2-(piperidin-1-yl)acetamido)-N-butyl-2-(substituted) benzamide derivatives were synthesized in which as structural features the 2-(1-pyrrolidinyl)- or 2-(1-piperidyl)acetylamino group or a diphenylether moiety are associated to a benzamide scaffold. Their binding affinity for human PrP(C) and inhibition of its conversion into PrP(Sc) were determined in vitro; moreover, the antiprion activity was assayed by inhibition of PrP(Sc) accumulation in scrapie-infected mouse neuroblastoma cells (ScN2a) and scrapie mouse brain (SMB) cells. The results clearly indicate the benzamide derivatives as attractive lead compounds for the development of potential therapeutic agents against prion disease.
KW  - Animals
KW  - Benzamides: chemical synthesis
KW  - Benzamides: chemistry
KW  - Benzamides: pharmacology
KW  - Cell Line
KW  - Dose-Response Relationship, Drug
KW  - Humans
KW  - Mice
KW  - Molecular Structure
KW  - Prions: antagonists & inhibitors
KW  - Prions: metabolism
KW  - Recombinant Proteins: antagonists & inhibitors
KW  - Recombinant Proteins: metabolism
KW  - Scrapie: drug therapy
KW  - Scrapie: metabolism
KW  - Structure-Activity Relationship
KW  - Benzamides (NLM Chemicals)
KW  - Prions (NLM Chemicals)
KW  - Recombinant Proteins (NLM Chemicals)
KW  - benzamide (NLM Chemicals)
LB  - PUB:(DE-HGF)16
C6  - pmid:22795751
DO  - DOI:10.1016/j.bmc.2012.06.026
UR  - https://pub.dzne.de/record/141238
ER  -