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Artigo Produção Nacional Revisado por pares
BIBTEX RIS

Structure–activity relationship of wedelolactone analogues: Structural requirements for inhibition of Na+,K+-ATPase and binding to the central benzodiazepine receptor

2006; Elsevier BV; Volume: 14; Issue: 23 Linguagem: Inglês

10.1016/j.bmc.2006.07.053

ISSN

1464-3391

Autores

Elisa Suzana Carneiro Pôças, Daniele V.S. Lopes, Alcides J. M. da Silva, Paulo Henrique Cotrim Pimenta, Fernanda Leitão, Chaquip D. Netto, Camilla D. Buarque, Flávia V. Brito, Paulo R. R. Costa, François Noël,

Tópico(s)

Traditional and Medicinal Uses of Annonaceae

Resumo

Coumestans 2a–i, bearing different patterns of substitution in A- and D-rings, were synthesized and evaluated as inhibitors of kidney Na+,K+-ATPase and ligands for the central benzodiazepine (BZP) receptor. The presence of a hydroxyl group in position 2 favours the effect on Na+,K+-ATPase but decreases the affinity for the BZP receptor, allowing the design of more selective molecules than the natural wedelolactone. On the other hand, the presence of a catechol in ring D is important for the effect on both molecular targets.

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