Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor
- Autores
- Escalante, Andrea Marta; Riera, Micaela Belen; Salazar, Mario Oscar; Furlan, Ricardo Luis Eugenio
- Año de publicación
- 2024
- Idioma
- inglés
- Tipo de recurso
- artículo
- Estado
- versión publicada
- Descripción
- Traditional methods for discovering bioactive compounds can be time-consuming and resource-intensive, often requiring extensive synthesis and evaluation. To address these challenges, thisstudy combines TLC-based assays with dithioacetal mixture-library preparation, enabling rapid and effective bioactivity screening. Tyrosinase, an enzyme crucial for melanin production and fruitbrowning, serves as a significant therapeutic target in this context. Despite the substantial potential of sulfur-containing compounds in medicinal chemistry, the use of dithioacetals in drug discoveryremains limited. In this study, two small libraries of dithioacetals, comprising more than 150 compounds, were prepared as mixturelibraries and screened on TLC by directly measuring tyrosinase activity on the plate surface. This approach facilitated the efficient preparation and identification of a potent, simple, and readily accessible dithioacetal inhibitor of tyrosinase, with the entire process being conducted on a low milligram scale.
Fil: Escalante, Andrea Marta. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas.; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
Fil: Riera, Micaela Belen. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina
Fil: Salazar, Mario Oscar. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
Fil: Furlan, Ricardo Luis Eugenio. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina - Materia
-
dithioacetal
effect-directed
tyrosinase-inhibitor
thin-layer-chromatography - Nivel de accesibilidad
- acceso embargado
- Condiciones de uso
- https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
- Repositorio
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/247759
Ver los metadatos del registro completo
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Effect‐Directed Synthesis of a Dithioacetal Tyrosinase InhibitorEscalante, Andrea MartaRiera, Micaela BelenSalazar, Mario OscarFurlan, Ricardo Luis Eugeniodithioacetaleffect-directedtyrosinase-inhibitorthin-layer-chromatographyhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Traditional methods for discovering bioactive compounds can be time-consuming and resource-intensive, often requiring extensive synthesis and evaluation. To address these challenges, thisstudy combines TLC-based assays with dithioacetal mixture-library preparation, enabling rapid and effective bioactivity screening. Tyrosinase, an enzyme crucial for melanin production and fruitbrowning, serves as a significant therapeutic target in this context. Despite the substantial potential of sulfur-containing compounds in medicinal chemistry, the use of dithioacetals in drug discoveryremains limited. In this study, two small libraries of dithioacetals, comprising more than 150 compounds, were prepared as mixturelibraries and screened on TLC by directly measuring tyrosinase activity on the plate surface. This approach facilitated the efficient preparation and identification of a potent, simple, and readily accessible dithioacetal inhibitor of tyrosinase, with the entire process being conducted on a low milligram scale.Fil: Escalante, Andrea Marta. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas.; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; ArgentinaFil: Riera, Micaela Belen. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; ArgentinaFil: Salazar, Mario Oscar. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; ArgentinaFil: Furlan, Ricardo Luis Eugenio. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; ArgentinaWiley VCH Verlag2024-10info:eu-repo/date/embargoEnd/2025-04-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/247759Escalante, Andrea Marta; Riera, Micaela Belen; Salazar, Mario Oscar; Furlan, Ricardo Luis Eugenio; Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor; Wiley VCH Verlag; European Journal of Organic Chemistry; 10-2024; 1-61434-193XCONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/ejoc.202401006info:eu-repo/semantics/altIdentifier/doi/10.1002/ejoc.202401006info:eu-repo/semantics/embargoedAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:37:20Zoai:ri.conicet.gov.ar:11336/247759instacron: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:34982025-09-29 10:37:20.274CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse |
dc.title.none.fl_str_mv |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
title |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
spellingShingle |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor Escalante, Andrea Marta dithioacetal effect-directed tyrosinase-inhibitor thin-layer-chromatography |
title_short |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
title_full |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
title_fullStr |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
title_full_unstemmed |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
title_sort |
Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor |
dc.creator.none.fl_str_mv |
Escalante, Andrea Marta Riera, Micaela Belen Salazar, Mario Oscar Furlan, Ricardo Luis Eugenio |
author |
Escalante, Andrea Marta |
author_facet |
Escalante, Andrea Marta Riera, Micaela Belen Salazar, Mario Oscar Furlan, Ricardo Luis Eugenio |
author_role |
author |
author2 |
Riera, Micaela Belen Salazar, Mario Oscar Furlan, Ricardo Luis Eugenio |
author2_role |
author author author |
dc.subject.none.fl_str_mv |
dithioacetal effect-directed tyrosinase-inhibitor thin-layer-chromatography |
topic |
dithioacetal effect-directed tyrosinase-inhibitor thin-layer-chromatography |
purl_subject.fl_str_mv |
https://purl.org/becyt/ford/1.4 https://purl.org/becyt/ford/1 |
dc.description.none.fl_txt_mv |
Traditional methods for discovering bioactive compounds can be time-consuming and resource-intensive, often requiring extensive synthesis and evaluation. To address these challenges, thisstudy combines TLC-based assays with dithioacetal mixture-library preparation, enabling rapid and effective bioactivity screening. Tyrosinase, an enzyme crucial for melanin production and fruitbrowning, serves as a significant therapeutic target in this context. Despite the substantial potential of sulfur-containing compounds in medicinal chemistry, the use of dithioacetals in drug discoveryremains limited. In this study, two small libraries of dithioacetals, comprising more than 150 compounds, were prepared as mixturelibraries and screened on TLC by directly measuring tyrosinase activity on the plate surface. This approach facilitated the efficient preparation and identification of a potent, simple, and readily accessible dithioacetal inhibitor of tyrosinase, with the entire process being conducted on a low milligram scale. Fil: Escalante, Andrea Marta. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas.; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina Fil: Riera, Micaela Belen. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina Fil: Salazar, Mario Oscar. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina Fil: Furlan, Ricardo Luis Eugenio. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina |
description |
Traditional methods for discovering bioactive compounds can be time-consuming and resource-intensive, often requiring extensive synthesis and evaluation. To address these challenges, thisstudy combines TLC-based assays with dithioacetal mixture-library preparation, enabling rapid and effective bioactivity screening. Tyrosinase, an enzyme crucial for melanin production and fruitbrowning, serves as a significant therapeutic target in this context. Despite the substantial potential of sulfur-containing compounds in medicinal chemistry, the use of dithioacetals in drug discoveryremains limited. In this study, two small libraries of dithioacetals, comprising more than 150 compounds, were prepared as mixturelibraries and screened on TLC by directly measuring tyrosinase activity on the plate surface. This approach facilitated the efficient preparation and identification of a potent, simple, and readily accessible dithioacetal inhibitor of tyrosinase, with the entire process being conducted on a low milligram scale. |
publishDate |
2024 |
dc.date.none.fl_str_mv |
2024-10 info:eu-repo/date/embargoEnd/2025-04-11 |
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/11336/247759 Escalante, Andrea Marta; Riera, Micaela Belen; Salazar, Mario Oscar; Furlan, Ricardo Luis Eugenio; Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor; Wiley VCH Verlag; European Journal of Organic Chemistry; 10-2024; 1-6 1434-193X CONICET Digital CONICET |
url |
http://hdl.handle.net/11336/247759 |
identifier_str_mv |
Escalante, Andrea Marta; Riera, Micaela Belen; Salazar, Mario Oscar; Furlan, Ricardo Luis Eugenio; Effect‐Directed Synthesis of a Dithioacetal Tyrosinase Inhibitor; Wiley VCH Verlag; European Journal of Organic Chemistry; 10-2024; 1-6 1434-193X CONICET Digital CONICET |
dc.language.none.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
info:eu-repo/semantics/altIdentifier/url/https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/ejoc.202401006 info:eu-repo/semantics/altIdentifier/doi/10.1002/ejoc.202401006 |
dc.rights.none.fl_str_mv |
info:eu-repo/semantics/embargoedAccess https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
eu_rights_str_mv |
embargoedAccess |
rights_invalid_str_mv |
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
dc.format.none.fl_str_mv |
application/pdf application/pdf application/pdf application/pdf |
dc.publisher.none.fl_str_mv |
Wiley VCH Verlag |
publisher.none.fl_str_mv |
Wiley VCH Verlag |
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 |
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1844614393325682688 |
score |
13.070432 |