916754-90-0Relevant articles and documents
Structure-activity relationship of wedelolactone analogues: Structural requirements for inhibition of Na+,K+-ATPase and binding to the central benzodiazepine receptor
Pocas, Elisa S.C.,Lopes, Daniele V.S.,da Silva, Alcides J.M.,Pimenta, Paulo H.C.,Leitao, Fernanda B.,Netto, Chaquip D.,Buarque, Camilla D.,Brito, Flavia V.,Costa, Paulo R.R.,Noel, Francois
, p. 7962 - 7966 (2007/10/03)
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.
