Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines

A series of 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines has been synthesized and evaluated for hypotensive activity. The QSAR studies indicate that resonance and hydrophobic parameters of the aryl substituents are important for hypotensive activity. The similar role of resonance parameter in describing the variance of 5-HT2A receptor binding affinities of these compounds suggests a possible role of 5-HT2A receptors in mediating the hypotensive action of title compounds.

Graphical abstractSynthesis and QSAR studies in a series of 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines for their hypotensive and 5-HT2A receptor binding affinities show that hydrophobicity and resonance parameters are important for the activities.Figure optionsDownload full-size imageDownload as PowerPoint slide