New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease

Autores
Biscussi, Brunella; Murray, Ana Paula
Año de publicación
2022
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In this work we present the microwave-assisted synthesis and in vitro acetylcholinesteraseinhibition of a series of new caffeine derivatives. The design of these new compounds was inspiredby the caffeine–pyrrolidine hybrids that act as AChE inhibitors and nAChR activators, previouslyreported by our group. All of the new caffeine analogs inhibited AChE. Among them, the compound2b (1,3-dimethyl-7-(6-(piperidin-1-yl)hexyl)-3,7-dihydro-1H-purine-2,6-dione) showed the strongesteffect (IC50 = 0.17 µM) on AChE, with higher potency than caffeine–pyrrolidine hybrids. Thesepreliminary studies suggest that these new compounds might be interesting multifunctional drugsdestined to stimulate cholinergic signage.
Fil: Biscussi, Brunella. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Química del Sur. Universidad Nacional del Sur. Departamento de Química. Instituto de Química del Sur; Argentina
Fil: Murray, Ana Paula. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Química del Sur. Universidad Nacional del Sur. Departamento de Química. Instituto de Química del Sur; Argentina
Materia
MICROWAVE-ASSISTED SYNTHESIS
CHOLINESTERASE INHIBITORS
ALZHEIMER'S DIASEASE
ACETYLCHOLINESTERASE
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/204374
Acceder
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network_name_str CONICET Digital (CONICET)
spelling New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s DiseaseBiscussi, BrunellaMurray, Ana PaulaMICROWAVE-ASSISTED SYNTHESISCHOLINESTERASE INHIBITORSALZHEIMER'S DIASEASEACETYLCHOLINESTERASEhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1In this work we present the microwave-assisted synthesis and in vitro acetylcholinesteraseinhibition of a series of new caffeine derivatives. The design of these new compounds was inspiredby the caffeine–pyrrolidine hybrids that act as AChE inhibitors and nAChR activators, previouslyreported by our group. All of the new caffeine analogs inhibited AChE. Among them, the compound2b (1,3-dimethyl-7-(6-(piperidin-1-yl)hexyl)-3,7-dihydro-1H-purine-2,6-dione) showed the strongesteffect (IC50 = 0.17 µM) on AChE, with higher potency than caffeine–pyrrolidine hybrids. Thesepreliminary studies suggest that these new compounds might be interesting multifunctional drugsdestined to stimulate cholinergic signage.Fil: Biscussi, Brunella. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Química del Sur. Universidad Nacional del Sur. Departamento de Química. Instituto de Química del Sur; ArgentinaFil: Murray, Ana Paula. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Química del Sur. Universidad Nacional del Sur. Departamento de Química. Instituto de Química del Sur; ArgentinaMultidisciplinary Digital Publishing Institute2022-11-14info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/204374Biscussi, Brunella; Murray, Ana Paula; New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease; Multidisciplinary Digital Publishing Institute ; Chemistry Proceedings; 12; 62; 14-11-2022; 1-52673-4583CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.3390/ecsoc-26-13578info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/2673-4583/12/1/62info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T10:04:10Zoai:ri.conicet.gov.ar:11336/204374instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-03 10:04:10.64CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
title New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
spellingShingle New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
Biscussi, Brunella
MICROWAVE-ASSISTED SYNTHESIS
CHOLINESTERASE INHIBITORS
ALZHEIMER'S DIASEASE
ACETYLCHOLINESTERASE
title_short New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
title_full New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
title_fullStr New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
title_full_unstemmed New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
title_sort New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease
dc.creator.none.fl_str_mv Biscussi, Brunella
Murray, Ana Paula
author Biscussi, Brunella
author_facet Biscussi, Brunella
Murray, Ana Paula
author_role author
author2 Murray, Ana Paula
author2_role author
dc.subject.none.fl_str_mv MICROWAVE-ASSISTED SYNTHESIS
CHOLINESTERASE INHIBITORS
ALZHEIMER'S DIASEASE
ACETYLCHOLINESTERASE
topic MICROWAVE-ASSISTED SYNTHESIS
CHOLINESTERASE INHIBITORS
ALZHEIMER'S DIASEASE
ACETYLCHOLINESTERASE
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv In this work we present the microwave-assisted synthesis and in vitro acetylcholinesteraseinhibition of a series of new caffeine derivatives. The design of these new compounds was inspiredby the caffeine–pyrrolidine hybrids that act as AChE inhibitors and nAChR activators, previouslyreported by our group. All of the new caffeine analogs inhibited AChE. Among them, the compound2b (1,3-dimethyl-7-(6-(piperidin-1-yl)hexyl)-3,7-dihydro-1H-purine-2,6-dione) showed the strongesteffect (IC50 = 0.17 µM) on AChE, with higher potency than caffeine–pyrrolidine hybrids. Thesepreliminary studies suggest that these new compounds might be interesting multifunctional drugsdestined to stimulate cholinergic signage.
Fil: Biscussi, Brunella. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Química del Sur. Universidad Nacional del Sur. Departamento de Química. Instituto de Química del Sur; Argentina
Fil: Murray, Ana Paula. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Química del Sur. Universidad Nacional del Sur. Departamento de Química. Instituto de Química del Sur; Argentina
description In this work we present the microwave-assisted synthesis and in vitro acetylcholinesteraseinhibition of a series of new caffeine derivatives. The design of these new compounds was inspiredby the caffeine–pyrrolidine hybrids that act as AChE inhibitors and nAChR activators, previouslyreported by our group. All of the new caffeine analogs inhibited AChE. Among them, the compound2b (1,3-dimethyl-7-(6-(piperidin-1-yl)hexyl)-3,7-dihydro-1H-purine-2,6-dione) showed the strongesteffect (IC50 = 0.17 µM) on AChE, with higher potency than caffeine–pyrrolidine hybrids. Thesepreliminary studies suggest that these new compounds might be interesting multifunctional drugsdestined to stimulate cholinergic signage.
publishDate 2022
dc.date.none.fl_str_mv 2022-11-14
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/204374
Biscussi, Brunella; Murray, Ana Paula; New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease; Multidisciplinary Digital Publishing Institute ; Chemistry Proceedings; 12; 62; 14-11-2022; 1-5
2673-4583
CONICET Digital
CONICET
url http://hdl.handle.net/11336/204374
identifier_str_mv Biscussi, Brunella; Murray, Ana Paula; New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimer’s Disease; Multidisciplinary Digital Publishing Institute ; Chemistry Proceedings; 12; 62; 14-11-2022; 1-5
2673-4583
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.3390/ecsoc-26-13578
info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/2673-4583/12/1/62
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Multidisciplinary Digital Publishing Institute
publisher.none.fl_str_mv Multidisciplinary Digital Publishing Institute
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1842269841510105088
score 13.13397

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