Paper
SYNTHESIS AND PHARMACOLOGY OF SOME BASIC ESTERS OF 3,4,5-TRIMETHOXYBENZOIC ACID.
Published Feb 1, 1964 · A. J. Vazakas, J. Doluisio
Journal of pharmaceutical sciences
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Abstract
A series of basic esters of 3,4,5-trimethoxybenzoic acid has been synthesized and the compounds evaluated for antihypertensive and local anesthetic activity. One of the compounds, a diamine ester prepared from N-methyl-N-phenyl-N′-propyl-ethylenediamine via a three-step synthesis, exhibited hypotensive activity following intravenous administration to normotensive dogs. No hypotensive activity was demonstrated following intraperitoneal administration to renal hypertensive rats. All but one of the compounds tested exhibited some degree of local anesthetic activity.
Basic esters of 3,4,5-trimethoxybenzoic acid show potential as antihypertensive agents and local anesthetics, with one showing hypotensive activity in dogs but no activity in rats.
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