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Título

Synthesis of a library of 3-oxopiperazinium and perhydro-3-oxo-1,4-diazepinium derivatives and identification of bioactive compounds

AutorMasip, Isabel; Ferrándiz-Huertas, Clotilde; García-Martínez, Carolina; Ferragut, José A.; Ferrer-Montiel, Antonio; Messeguer Peypoch, Ángel
Palabras clave3-Oxopiperazinium and Perhydro-3-oxo-1,4-diazepinium
Identification of bioactive compounds
Receptors
Library compounds
Fecha de publicación12-ene-2004
EditorAmerican Chemical Society
CitaciónJournal of Combinatorial Chemistry 6(1): 135-141 (2004)
ResumenThe design and synthesis of a library of novel families of 3-oxopiperazinium and perhydro-3-oxo-1,4-diazepinium derivatives is reported. The library was composed of 44 3-oxopiperazinium derivatives (11 of these compounds had a spiranic skeleton) and 22 perhydro-3-oxo-1,4-diazepinium compounds. The synthetic procedure involved a 6-step sequence carried out in solution, along with the use of solid-phase linked scavengers and microwave activation for the rapid removal of the excess of amine reagents. A final cyclization step performed under mild conditions led to the charged heterocyclic moiety. Screening of this library in two biological assays identified active compounds that inhibit the activity of the vanilloid receptor TRPV1 and modulators of the multidrug resistance phenomenon. Thus, this synthetic sequence represents a facile and convenient entry to unprecedented libraries of this sort of tetraalkylammonium derivatives that may be of use for identification of novel scaffolds of diverse biological activity.
Descripción7 pages, 5 figures, 1 scheme, 1 table.-- PMID: 14714997 [PubMed].-- Available online Nov 18, 2003.-- Supporting information available at: http://pubs.acs.org/doi/suppl/10.1021/cc030002q
Versión del editorhttp://dx.doi.org/10.1021/cc030002q
URIhttp://hdl.handle.net/10261/17928
DOI10.1021/cc030002q
ISSN1520-4766 (Print)
1520-4774 (Online)
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