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Synthesis, anxiolytic and antihypertensive activity of 1-aryloxy-3-(N4-substituted piperazinyl ) propan-2-ols as aryloxypropanolamines | Abstract
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Abstract

Synthesis, anxiolytic and antihypertensive activity of 1-aryloxy-3-(N4-substituted piperazinyl ) propan-2-ols as aryloxypropanolamines

Author(s): Ganesh B. Gajeli and Sanjay B. Wagha

Aryloxypropanolamines have an important role in the treatment of several cardiovascular disorders and are one of the most potent antihypertensive agents. A series of 1-aryloxy-3-(N4-substituted piperazinyl) propan-2-ols as aryloxypropanolamine were synthesized and evaluated for anxiolytic activity and antihypertensive activity. The structures of synthesized compounds were confirmed by IR, 1H NMR and Mass spectroscopy.1-aryloxy-3-(N4- substituted Piperazinyl) propan-2-ols were synthesized by reaction of various phenols (1a-c) with epichlorhydrin to form 1-aryloxy-2,3-epoxypropane.These epoxides on condensation with various substituted piperazines resulted in derivatives of aryloxypropanolamine compounds (4a-i) and were evaluated for anxiolytic activity by Elevated Plus Maze and antihypertensive activity by Tail Cuff technique. Out of nine (4a-i) compounds , Compound 4e [1-(2- naphthyloxy)-3-(N4-ethyl piperazinyl) propan-2-ol], 4i [1-(phenoxy)-3-(N4-hydroxyethyl piperazinyl)] propan-2-ol were found to be most active as anxiolytic agent whereas compound 4a [1-(1 -Naphthyloxy)-3-(N4-methyl piperazinyl) propan-2-ol] was possessing maximum antihypertensive activity.