Synthesis and Characterization of some Xanthonoxypropanolamines and Evaluation of their Toxicity

Abstract

In the present work Synthesis and Characterization of some Xanthonoxypropanolamines and newlineEvaluation of their Toxicity we have synthesized and characterized new Xanthone newlinederivatives bearing xanthon and propanolamine through etheral linkage and and evaluated for newlinetheir antihypertensive activity against methyl prednisolone acetate induced hypertensive newlinealbino wistar rats by using Digital LE-S100 Blood Pressure Meter in Tail-cuff method. The newlinenovel compounds were also evaluated for their toxicity. A total of 3 new xanthone derivatives newlinewere synthesized by the scheme (Scheme 1) and screened for their antihypertensive activity newlinealong with toxicity evaluation. The first part based on exhaustive literature survey on newlinebiologically active xanthone and propanolamines in relation to antihypertensive activity. The newlinesecond part deals with the rational design of the targeted compounds with reported beta newlineblockers considering xanthone and propanolamine as pharmacophoric group for newlineantihypertensive activity (Figure 1). Xanthones are structurally related to napthol and are newlineligands for beta receptors. Additionally, propanolamine being an important scaffold in newlinevarious biologically active molecules is widely explored for the development of newlineantihypertensive agents. The third part is related with the synthesis of xanthone derivatives newlinebearing propanolamine as shown in Scheme 1. Modern analytical techniques (IR, NMR and newlineMass) and elemental analysis were applied to establish the structure of the newly synthesized newlinecompounds. All the compounds were investigated for toxicity and pharmacokinetic newlineparameters. It was observed during the studies that these novel compounds i.e. 1a, 1b, and 2 newlinehave greater antihypertensive activity in comparison to standard drugs Propranolol and newlineAtenolol, as these compounds showed greater percentage of reduction in both systolic and newlinemean blood pressure. The compounds did not exhibit any toxicity during study, as no death newlineof any rat occurred during antihypertensive screening study and the level of different newlinebiochemical paramet