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001     141238
005     20240321220932.0
024 7 _ |a 10.1016/j.bmc.2012.06.026
|2 doi
024 7 _ |a pmid:22795751
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024 7 _ |a 0968-0896
|2 ISSN
024 7 _ |a 1464-3391
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024 7 _ |a altmetric:844061
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037 _ _ |a DZNE-2020-07560
041 _ _ |a English
082 _ _ |a 610
100 1 _ |a Fiorino, Ferdinando
|b 0
245 _ _ |a Synthesis of benzamide derivatives and their evaluation as antiprion agents.
260 _ _ |a Amsterdam [u.a.]
|c 2012
|b Elsevier
264 _ 1 |3 print
|2 Crossref
|b Elsevier BV
|c 2012-08-01
336 7 _ |a article
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336 7 _ |a Output Types/Journal article
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336 7 _ |a Journal Article
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336 7 _ |a ARTICLE
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336 7 _ |a Journal Article
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520 _ _ |a 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.
536 _ _ |a 342 - Disease Mechanisms and Model Systems (POF3-342)
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542 _ _ |i 2012-08-01
|2 Crossref
|u https://www.elsevier.com/tdm/userlicense/1.0/
588 _ _ |a Dataset connected to CrossRef, PubMed,
650 _ 7 |a Benzamides
|2 NLM Chemicals
650 _ 7 |a Prions
|2 NLM Chemicals
650 _ 7 |a Recombinant Proteins
|2 NLM Chemicals
650 _ 7 |a benzamide
|0 6X80438640
|2 NLM Chemicals
650 _ 2 |a Animals
|2 MeSH
650 _ 2 |a Benzamides: chemical synthesis
|2 MeSH
650 _ 2 |a Benzamides: chemistry
|2 MeSH
650 _ 2 |a Benzamides: pharmacology
|2 MeSH
650 _ 2 |a Cell Line
|2 MeSH
650 _ 2 |a Dose-Response Relationship, Drug
|2 MeSH
650 _ 2 |a Humans
|2 MeSH
650 _ 2 |a Mice
|2 MeSH
650 _ 2 |a Molecular Structure
|2 MeSH
650 _ 2 |a Prions: antagonists & inhibitors
|2 MeSH
650 _ 2 |a Prions: metabolism
|2 MeSH
650 _ 2 |a Recombinant Proteins: antagonists & inhibitors
|2 MeSH
650 _ 2 |a Recombinant Proteins: metabolism
|2 MeSH
650 _ 2 |a Scrapie: drug therapy
|2 MeSH
650 _ 2 |a Scrapie: metabolism
|2 MeSH
650 _ 2 |a Structure-Activity Relationship
|2 MeSH
700 1 _ |a Eiden, Martin
|b 1
700 1 _ |a Giese, Armin
|0 P:(DE-HGF)0
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700 1 _ |a Severino, Beatrice
|b 3
700 1 _ |a Esposito, Antonella
|b 4
700 1 _ |a Groschup, Martin H
|b 5
700 1 _ |a Perissutti, Elisa
|b 6
700 1 _ |a Magli, Elisa
|b 7
700 1 _ |a Incisivo, Giuseppina Maria
|b 8
700 1 _ |a Ciano, Antonio
|b 9
700 1 _ |a Frecentese, Francesco
|b 10
700 1 _ |a Kretzschmar, Hans A
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700 1 _ |a Wagner, Jens
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700 1 _ |a Santagada, Vincenzo
|b 13
700 1 _ |a Caliendo, Giuseppe
|0 P:(DE-HGF)0
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|e Corresponding author
773 1 8 |a 10.1016/j.bmc.2012.06.026
|b : Elsevier BV, 2012-08-01
|n 16
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|t Bioorganic & Medicinal Chemistry
|v 20
|y 2012
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773 _ _ |a 10.1016/j.bmc.2012.06.026
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910 1 _ |a Deutsches Zentrum für Neurodegenerative Erkrankungen
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