Journal Article

DZNE-2020-07560

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Synthesis of benzamide derivatives and their evaluation as antiprion agents.

Fiorino, F. ; Eiden, M. ; Giese, A. ; Severino, B. ; Esposito, A. ; Groschup, M. H. ; Perissutti, E. ; Magli, E. ; Incisivo, G. M. ; Ciano, A. ; Frecentese, F. ; Kretzschmar, H. A. ; Wagner, J.DZNE* ; Santagada, V. ; Caliendo, G. (Corresponding author)

2012
Elsevier Amsterdam [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.bmc.2012.06.026

Abstract: 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.

Keyword(s): Animals (MeSH) ; Benzamides: chemical synthesis (MeSH) ; Benzamides: chemistry (MeSH) ; Benzamides: pharmacology (MeSH) ; Cell Line (MeSH) ; Dose-Response Relationship, Drug (MeSH) ; Humans (MeSH) ; Mice (MeSH) ; Molecular Structure (MeSH) ; Prions: antagonists & inhibitors (MeSH) ; Prions: metabolism (MeSH) ; Recombinant Proteins: antagonists & inhibitors (MeSH) ; Recombinant Proteins: metabolism (MeSH) ; Scrapie: drug therapy (MeSH) ; Scrapie: metabolism (MeSH) ; Structure-Activity Relationship (MeSH) ; Benzamides ; Prions ; Recombinant Proteins ; benzamide

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Contributing Institute(s):

1. Neuroimmunology and Imaging (AG Fuhrmann)

Research Program(s):

1. 342 - Disease Mechanisms and Model Systems (POF3-342) (POF3-342)

Appears in the scientific report 2012

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Database coverage:
; BIOSIS Previews ; Clarivate Analytics Master Journal List ; Current Contents - Life Sciences ; Ebsco Academic Search ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; Nationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Web of Science Core Collection

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