Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives

In this report we disclose the synthesis, vasodilatory activity, and identification of bioactive conformation of new N-acylhydrazone and N-methyl-N-acylhydrazone derivatives, structurally designed by bioisosteric replacements of previously described cardioactive compounds LASSBio-294 and its N-methyl derivative LASSBio-785. Some of these novel derivatives presented improved vasorelaxant properties, being new cardiovascular drug candidates.

Graphical abstractIn this paper is described the bioactive conformation of new N-acylhydrazone (NAH) derivatives, bioisostere of the previously described potent cardioactive compound LASSBio-294. These novel derivatives – N-methyl homologues – presented important vasodilator properties.Figure optionsDownload full-size imageDownload as PowerPoint slide