Novel analogues of Istaroxime, a potent inhibitor of Na(+),K(+)-ATPase: Synthesis, structure-activity relationship and 3D-quantitative structure-activity relationship of derivatives at position 6 on the androstane scaffold

We report the synthesis and biological properties of novel analogues of Istaroxime acting as positive inotropic compounds through the inhibition of the Na(+),K(+)-ATPase. We explored the chemical space around the position 6 of the steroidalscaffold by changing the functional groups at that position and maintaining a basic oximic chain in position 3.

Mauro Gobbini, Silvia Armaroli, Leonardo Banfi, Alessandra Benicchio, Giulio Carzana, Giorgio Fedrizzi, Patrizia Ferrari, Giuseppe Giacalone, Michele Giubileo, Giuseppe Marazzi, Rosella Micheletti, Barbara Moro, Marco Pozzi, Piero Enrico Scotti, Marco Torri, Alberto Cerri
June 15, 2010
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