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

Autor: Pôças ES; Departamento de Farmacologia Básica e Clínica, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, RJ 21941-590, Brazil., Lopes DV, da Silva AJ, Pimenta PH, Leitão FB, Netto CD, Buarque CD, Brito FV, Costa PR, Noël F
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2006 Dec 01; Vol. 14 (23), pp. 7962-6. Date of Electronic Publication: 2006 Aug 30.
DOI: 10.1016/j.bmc.2006.07.053
Abstrakt: 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.
Databáze: MEDLINE
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