Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation.

Panek, Dawid; Wieckowska, Anna; Wichur, Tomasz; Bajda, Marek; Godyn, Justyna; Jonczyk, Jakub; Mika, Kamil; Janockova, Jana; Soukup, Ondrej; Knez, Damijan; Korabecny, Jan; Gobec, Stanislav; Malawska, Barbara

Panek, Dawid; Wieckowska, Anna; Wichur, Tomasz; Bajda, Marek; Godyn, Justyna; Jonczyk, Jakub; Mika, Kamil; Janockova, Jana; Soukup, Ondrej; Knez, Damijan; Korabecny, Jan; Gobec, Stanislav; Malawska, Barbara.

Afiliación

Panek D; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Wieckowska A; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Wichur T; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Bajda M; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Godyn J; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Jonczyk J; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Mika K; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Janockova J; Biomedical Research Centre, University Hospital Hradec Kralove, Czech Republic.
Soukup O; Biomedical Research Centre, University Hospital Hradec Kralove, Czech Republic.
Knez D; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia.
Korabecny J; Biomedical Research Centre, University Hospital Hradec Kralove, Czech Republic.
Gobec S; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia.
Malawska B; Department of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland. Electronic address: mfmalaws@cyf-kr.edu.pl.

Eur J Med Chem ; 125: 676-695, 2017 Jan 05.

Article en En | MEDLINE | ID: mdl-27721153

Asunto(s)

Aminas/química; Aminas/farmacología; Ftalimidas/química; Ftalimidas/farmacología; Sacarina/química; Sacarina/farmacología; Secretasas de la Proteína Precursora del Amiloide/metabolismo; Péptidos beta-Amiloides/metabolismo; Sitios de Unión; Barrera Hematoencefálica/efectos de los fármacos; Colinesterasas/metabolismo; Sistemas de Liberación de Medicamentos; Diseño de Fármacos; Inhibidores Enzimáticos/síntesis química; Inhibidores Enzimáticos/química; Inhibidores Enzimáticos/farmacología; Humanos; Concentración 50 Inhibidora; Estructura Molecular; Fragmentos de Péptidos/metabolismo; Ftalimidas/síntesis química; Agregación Patológica de Proteínas; Unión Proteica/efectos de los fármacos; Sacarina/síntesis química

Palabras clave

Acetylcholinesterase inhibitors; Alzheimer's disease; Aß aggregation; BACE1 inhibitors; Molecular docking; Multifunctional agents

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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Ftalimidas / Sacarina / Aminas Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2017 Tipo del documento: Article País de afiliación: Polonia

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