Tacrine-xanomeline and tacrine-iperoxo hybrid ligands: Synthesis and biological evaluation at acetylcholinesterase and M<sub>1</sub> muscarinic acetylcholine receptors.

Maspero, Marco; Volpato, Daniela; Cirillo, Davide; Yuan Chen, Natalia; Messerer, Regina; Sotriffer, Christoph; De Amici, Marco; Holzgrabe, Ulrike; Dallanoce, Clelia

Tacrine-xanomeline and tacrine-iperoxo hybrid ligands: Synthesis and biological evaluation at acetylcholinesterase and M₁ muscarinic acetylcholine receptors.

Maspero, Marco; Volpato, Daniela; Cirillo, Davide; Yuan Chen, Natalia; Messerer, Regina; Sotriffer, Christoph; De Amici, Marco; Holzgrabe, Ulrike; Dallanoce, Clelia.

Maspero M; Department of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.
Volpato D; Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
Cirillo D; Department of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.
Yuan Chen N; Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
Messerer R; Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
Sotriffer C; Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
De Amici M; Department of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.
Holzgrabe U; Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany. Electronic address: ulrike.holzgrabe@uni-wuerzburg.de.
Dallanoce C; Department of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy. Electronic address: clelia.dallanoce@unimi.it.

Bioorg Chem ; 96: 103633, 2020 03.

Article en En | MEDLINE | ID: mdl-32032848

Asunto(s)

Inhibidores de la Colinesterasa/farmacología; Isoxazoles/farmacología; Piridinas/farmacología; Compuestos de Amonio Cuaternario/farmacología; Receptor Muscarínico M1/metabolismo; Tacrina/farmacología; Tiadiazoles/farmacología; Acetilcolinesterasa/metabolismo; Regulación Alostérica/efectos de los fármacos; Animales; Células CHO; Inhibidores de la Colinesterasa/química; Cricetulus; Electrophorus; Humanos; Isoxazoles/síntesis química; Isoxazoles/química; Ligandos; Simulación del Acoplamiento Molecular; Piridinas/síntesis química; Piridinas/química; Compuestos de Amonio Cuaternario/síntesis química; Compuestos de Amonio Cuaternario/química; Receptor Muscarínico M1/agonistas; Tacrina/análogos & derivados; Tacrina/síntesis química; Tiadiazoles/síntesis química; Tiadiazoles/química

Palabras clave

Allosteric modulation; Bitopic ligands; Ellman's assay; Inositol monophosphate; Iperoxo; M(1) muscarinic acetylcholine receptor; Multitarget compounds; Phospholipase C; Tacrine; Xanomeline

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridinas / Tacrina / Tiadiazoles / Inhibidores de la Colinesterasa / Receptor Muscarínico M1 / Compuestos de Amonio Cuaternario / Isoxazoles Límite: Animals / Humans Idioma: En Año: 2020 Tipo del documento: Article

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