Novel Analogues of Istaroxime, a Potent Inhibitor of Na+, K+-ATPase: Synthesis and Structure− Activity Relationship†

…, G Marazzi, R Micheletti, B Moro, M Pozzi…

Index: Gobbini, Mauro; Armaroli, Silvia; Banfi, Leonardo; Benicchio, Alessandra; Carzana, Giulio; Fedrizzi, Giorgio; Ferrari, Patrizia; Giacalone, Giuseppe; Giubileo, Michele; Marazzi, Giuseppe; Micheletti, Rosella; Moro, Barbara; Pozzi, Marco; Scotti, Piero Enrico; Torri, Marco; Cerri, Alberto Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4601 - 4608

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Citation Number: 13

Abstract

We report the synthesis and biological properties of novel inhibitors of the Na+, K+-ATPase as positive inotropic compounds. Following our previously described model from which Istaroxime was generated, the 5α, 14α-androstane skeleton was used as a scaffold to study the space around the basic chain of our lead compound. Some compounds demonstrated higher potencies than Istaroxime on the receptor and the (E)-3-[(R)-3-pyrrolidinyl] oxime ...