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TitleDiels-alder cycloaddition in the synthesis of 1-azafagomine, analogs, and derivatives as glycosidase inhibitors
Author(s)Salgueiro, D. A. L.
Sousa, Cristina
Fortes, A. Gil
Alves, M. José
Biological activity
Diels-alder cycloaddition
Glycosidase inhibitors
Monocyclic analogs
Issue date2012
PublisherBentham Science Publishers
JournalMini Reviews in Medicinal Chemistry
Abstract(s)This comprehensive review deals with the synthesis of 1-azafagomine, analogs, and derivatives having the Diels-Alder cycloaddition as the key step. Most of the compounds referred are racemic or have been resolved by lipase transesterification. There are two asymmetric cycloadditions leading to 1-azafagomine or to an analog. In one case both enantiomers of 1-azafagomine were prepared together with a pair of derivatives. The study comprises glycosidase inhibition studies of the target compounds to a set of glycosidic enzymes, and evidenced molecular features that enhance or diminish their activity as glycosidase inhibitors.
AccessOpen access
Appears in Collections:CDQuim - Artigos (Papers)

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