Journal of China Pharmaceutical University 2001;(3):180-184

Synthesis and Antihypertensive Activity of 1-Phenylethyl(or 3,4-Dimethyloxyphenylethyl)-4-substituted Aryloxypiperidines

Weifang TANG ; Peizhou NI ; Lin XIA ; Jihua FU

Country

China

Language

Chinese

Abstract

AIM The purpose is to make a search for new antihypertensive agents with higher activity and lower side effect. METHODS As DDPH a lead compound, ten 1-Phenylethyl (or 3,4-dimethyloxyphenylethyl)-4-substituted aryloxypiperidine compounds were designed and synthesized, keeping the two structural fragments of DDPH: phenylethylamine and aryloxyalkylamine. Their structures were confirmed by Elemental Analysis, IR, 1H-NMR and Mass Spectrum. RESULTS The majority of the compounds possessed potent antihypertensive activity and the antihypertensive effect of I3 and I4 was stronger than that of DDPH. CONCLUSION The experimental results were accordant with designed thought and provided useful information for modifying the structure of DDPH deeply.