141238 20240321220932.0 10.1016/j.bmc.2012.06.026 doi pmid:22795751 pmid 0968-0896 ISSN 1464-3391 ISSN altmetric:844061 altmetric DZNE-2020-07560 English 610 Fiorino, Ferdinando 0 Synthesis of benzamide derivatives and their evaluation as antiprion agents. Amsterdam [u.a.] 2012 Elsevier print Crossref Elsevier BV 2012-08-01 article DRIVER Output Types/Journal article DataCite Journal Article journal journal PUB:(DE-HGF)16 1709816019_6142 PUB:(DE-HGF) ARTICLE BibTeX JOURNAL_ARTICLE ORCID Journal Article 0 EndNote 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. 342 - Disease Mechanisms and Model Systems (POF3-342) G:(DE-HGF)POF3-342 POF3-342 POF III 0 2012-08-01 Crossref https://www.elsevier.com/tdm/userlicense/1.0/ Dataset connected to CrossRef, PubMed, Benzamides NLM Chemicals Prions NLM Chemicals Recombinant Proteins NLM Chemicals benzamide 6X80438640 NLM Chemicals 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 Eiden, Martin 1 Giese, Armin P:(DE-HGF)0 2 Severino, Beatrice 3 Esposito, Antonella 4 Groschup, Martin H 5 Perissutti, Elisa 6 Magli, Elisa 7 Incisivo, Giuseppina Maria 8 Ciano, Antonio 9 Frecentese, Francesco 10 Kretzschmar, Hans A P:(DE-HGF)0 11 Wagner, Jens P:(DE-2719)2662292 12 dzne Santagada, Vincenzo 13 Caliendo, Giuseppe P:(DE-HGF)0 14 Corresponding author 10.1016/j.bmc.2012.06.026 : Elsevier BV, 2012-08-01 16 5001-5011 journal-article Crossref Bioorganic & Medicinal Chemistry 20 2012 0968-0896 10.1016/j.bmc.2012.06.026 Vol. 20, no. 16, p. 5001 - 5011 PERI:(DE-600)1501507-5 16 20:16<5001 - 5011 5001-5011 Bioorganic & medicinal chemistry 20 2012 0968-0896 http://pub.dzne.de/record/141238/files/DZNE-2020-07560_Restricted.pdf http://pub.dzne.de/record/141238/files/DZNE-2020-07560_Restricted.pdf?subformat=pdfa pdfa VDB oai:pub.dzne.de:141238 Deutsches Zentrum für Neurodegenerative Erkrankungen I:(DE-588)1065079516 DZNE 12 P:(DE-2719)2662292 DE-HGF Gesundheit Erkrankungen des Nervensystems G:(DE-HGF)POF3-340 G:(DE-HGF)POF3-342 G:(DE-HGF)POF3 G:(DE-HGF)POF3-300 G:(DE-HGF)POF Disease Mechanisms and Model Systems 0 2012 Nationallizenz StatID:(DE-HGF)0420 StatID DBCoverage StatID:(DE-HGF)0200 StatID SCOPUS DBCoverage StatID:(DE-HGF)0300 StatID Medline DBCoverage StatID:(DE-HGF)0310 StatID NCBI Molecular Biology Database JCR StatID:(DE-HGF)0100 StatID BIOORGAN MED CHEM : 2017 DBCoverage StatID:(DE-HGF)0600 StatID Ebsco Academic Search Peer Review StatID:(DE-HGF)0030 StatID ASC DBCoverage StatID:(DE-HGF)0199 StatID Clarivate Analytics Master Journal List WoS StatID:(DE-HGF)0110 StatID Science Citation Index DBCoverage StatID:(DE-HGF)0150 StatID Web of Science Core Collection WoS StatID:(DE-HGF)0111 StatID Science Citation Index Expanded DBCoverage StatID:(DE-HGF)1030 StatID Current Contents - Life Sciences DBCoverage StatID:(DE-HGF)1050 StatID BIOSIS Previews IF < 5 StatID:(DE-HGF)9900 StatID I:(DE-2719)1011004 AG Fuhrmann Neuroimmunology and Imaging 0 journal VDB I:(DE-2719)1011004 UNRESTRICTED