Design, synthesis, and evaluation of new series of Imperatorin analogs with potential vasodilatory activity

Journal of Asian Natural Products Research
Ya-Jing HouHuai-Zhen He

Abstract

Two series of imperatorin analogs were synthesized based on our previous research and evaluated for their vasodilatation activities on in vitro rat mesenteric artery, basilar artery, and renal artery ring models. Target compounds were characterized by infrared, 1H NMR, and mass spectra. Most derivatives possessed significant vasodilatory activity on the mesenteric artery, and compound 3a exhibited favorable and broad vasodilatation activities on three kinds of rat artery ring models. The pharmacological results indicated that introducing nitrogen-contained ring in side chain or large steric hindrance at the distal end could increase the vasodilatory activity. Further, replacement of oxygen atom (-O-) in the skeleton of furocoumarin derivatives with nitrogen (-NH-) could cause the decrease of vasodilatory activity. The molecular docking also indicated that compound 3a showed a best affinity with α-1C receptor (PDB ID: 3G43). All these results suggested compound 3a would be a potential vasodilatory agent for hypertension.

References

Apr 11, 2003·Lancet·Mariella AnselmiGianni Tognoni
May 21, 2003·Hypertension·Claude LenfantUNKNOWN Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure
Jun 26, 2004·The Journal of Biological Chemistry·Rocío SanchoEduardo Muñoz
Jul 11, 2009·European Journal of Medicinal Chemistry·Ranju BansalCarmen de la Calle
Aug 31, 2010·Archives of Pharmacal Research·Jingjing PanLangchong He
Aug 14, 2012·Lancet·M Mohsen Ibrahim, Albertino Damasceno

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Methods Mentioned

BETA
column chromatography

Software Mentioned

Sulflex - Dock Mode of Sybyl - X

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