Design and Synthesis of an Aniline Derivative with Biological Activity on Heart Failure.

BACKGROUND: Several compounds have been synthesized as a therapeutic alternative for heart failure; however, its preparation requires special conditions. OBJECTIVE: The aim of this study, was to synthesize some aniline derivatives (4-9) from 3- ethynylaniline to evaluate their biological activity against heart failure. METHODS: The synthesis of aniline derivatives involved a series of reactions such as etherification, addition, and cyclization. The structure of all compounds obtained was confirmed by spectroscopic and spectrometric methods. In addition, to evaluate the biological activity of compounds, an ischemia/reperfusion injury model was used. RESULTS: The results showed that compound 8 decreases heart failure, which translates into a decrease in the infarction area compared to compounds 4-7 and 9. CONCLUSION: This study reports a facile method for the preparation of aniline derivatives. This method offers some advantages such as; a simple procedure, low cost, and easy work up. In addition, compound 8 showed an interesting biological activity against heart failure. This phenomenon is particularly interesting because the biological activity induced by this compound could involve a molecular mechanism that is different from other drugs used for the treatment of heart failure.

Effective synthesis of a hexacyclic-steroid derivative from 4-hydroxyestrone.

Several studies have been reported for the preparation of hexacyclic-steroid derivatives; however, some reagents are expensive and require special conditions for handling. In this way, the objective of this study was to synthesize a hexacyclic-steroid derivative from 4-hydroxyestrone. The chemical structure was evaluated through both 1H NMR and 13C NMR spectroscopic analysis. The results showed good performance of the hexacyclic-steroid derivative. In conclusion in this study, an easy method for the preparation of the hexacyclic-steroid derivative is reported.

Design and synthesis of a new furan-steroid-propanone derivative using some chemical strategies.

There are several reports for the preparation of furan derivatives using some protocols which requires special conditions. In this way, the aim of this study was to synthesize a new furan-steroid-propanone derivative from both 17α-ethynylestradiol and 2-nitro-17α-ethynylestradiol using some series of reactions such as aldolization, 2 + 2 addition and etherification. The chemical structure was evaluated through both 1H NMR and 13C NMR spectroscopic analysis. The results showed a good yielding from furan-steroid derivative. In conclusion, this investigation provides a facile synthesis of a new furan-steroid-propanone derivative, using some reagents which are not expensive and do not require special conditions for handling.

Design and synthesis of two new steroid derivatives with biological activity on heart failure via the M2-muscarinic receptor activation.

Several drugs have been prepared to treat of heart failure using some protocols which require dangerous reagents and specific conditions. The aim of this study was to synthesize a series of steroid derivatives (compounds 2 to 18) using some chemical strategies. The biological activity of steroid derivatives against heart failure was evaluated using an ischemia/reperfusion model. In addition, the effect exerted by compounds 4 or 5 on left ventricular pressure was evaluated in the absence or presence of yohimbine, butaxamine and methoctramine. The results showed that 1) both compounds 4 or 5 significantly decrease the heart failure (translated as infarct area) compared with the compounds 2, 3 and 6-18. In addition, the compound 4 and 5 decreased the left ventricular pressure in a dose-dependent manner and this effect was significantly inhibited in the presence of methoctramine (p = 005). In conclusion, the compounds 4 or 5 decrease both the infarct area and left ventricular pressure via M2-muscarinic receptor activation.