Why the study?
Several steroid derivatives have been prepared as inotropic drugs, but few reports exist on azetidine-steroid derivatives with inotropic activity.
Do azetidine-steroid derivatives improve left ventricular pressure in a heart failure model?
Do azetidine-steroid derivatives improve left ventricular pressure in a heart failure model?
A newly synthesized azetidine-steroid derivative (compound 3) demonstrates positive inotropic effects by increasing left ventricular pressure in a preclinical heart failure model.
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Hypothesis-generating for azetidine-steroids as inotropes; leaves open any clinical role pending validation.
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.
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Lauro et al. (2020) studied this question.
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