Design and synthesis of new azetidine-steroid derivative with inotropic activity in a heart failure model

Abstract

Several steroid derivatives have prepared as inotropic drugs; however, there are few reports on azetidine-steroid derivatives with inotropic activity. The aim of this study was to synthesize four azetidine-steroid derivatives (compounds 3 to 6) to evaluate their biological activity on left ventricular pressure. The first stage was achieved by preparation of azetidine-derivatives using reactions of etherification and addition. The second stage involves the evaluation of biological activity from azetidine derivatives on left ventricular pressure in a heart failure model using estrone as control. The results showed that only compound 3 increases left ventricular pressure compared with estrone, compounds 2 and 4 to 6. In conclusion, the positive inotropic effect exerted by compound 3 depends on the functional groups involved in their Chemical structure.