Thymidine- and AZT-linked 5-(1,3-dioxoalkyl)tetrazoles and 4-(1,3-dioxoalkyl)-1,2,3-triazoles

N3 of thymidine and of 3′-azido-3′-deoxythymidine (AZT) has been linked to a tetrazole ring by condensation of nucleoside-derived 2-oxonitriles with the lithium salt of 5-acetyl-1-(4-fluorobenzyl)tetrazole (obtained by a 'click' reaction). 4-Acetyl-1,2,3-triazole, also prepared by a Cu-cat...

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Detalles Bibliográficos
Autores: Bosch Hereu, Lluís, Delelis, Olivier, Subra, Frédéric, Deprez, Eric, Witvrow, Myriam, Vilarrasa i Llorens, Jaume
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2012
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/158701
Acceso en línea:https://hdl.handle.net/2445/158701
Access Level:acceso abierto
Palabra clave:VIH (Virus)
Inhibidors de la integrasa
Integrase inhibitors
HIV (Viruses)
Descripción
Sumario:N3 of thymidine and of 3′-azido-3′-deoxythymidine (AZT) has been linked to a tetrazole ring by condensation of nucleoside-derived 2-oxonitriles with the lithium salt of 5-acetyl-1-(4-fluorobenzyl)tetrazole (obtained by a 'click' reaction). 4-Acetyl-1,2,3-triazole, also prepared by a Cu-catalysed cycloaddition, has been similarly linked. A route for the conjugation of NRTIs with pharmacophoric elements of integrase inhibitors (INIs) has thus been disclosed.