Synthesis And In Vitro Activiites On Anti-platelet Aggregation Of N,N’-di(3-substituted-phenyi)-4-methoxy Benzene-1,3-disulfonamides

In order to find more effective,low toxically and side-effect-free anti-platelet aggregationnovel drugs,we have designed and synthesized fifteen3-substituted phenyl series.Comparingdifferent the3-position of a substituted phenyl group against the influence of plateletaggregation activity,and2-substituted phenyl series related comparison. The results as aboveprovide some important references for our laboratory to research new drugs.Compound PN416that is4-methoxybenzene-N,N’-diphenyl-1,3-disulfonamide waschosen as a leading compound, instead of3-methyl aniline structure with a series of3-substituted anilines:anisole as raw materials, reaction with chlorosulfonic acid reactionprepared directly important intermediates4-methoxy-1,3-benzenedisulfonyl chloride byliterature methods, and aminolysis reaction of this intermediate with the3-substitutedanilines.The15objective compound (416-430) were designed and synthesized. And theirchemical structures were confirmed by1H-NMR and IR and the anti-platelet aggregationactivity was tested through Born’s turbidity method. The results shows that of which sevencompounds have higher activities than Picotamide and compound PN424has highestactivity.Contrast the activities of3-substituted phenyl series with structural similarcompounds of2-substituted phenyl series, the results show that the avtivities of thecompounds in two series are similar each other.(PN102>PN421,PN17<PN422,PN8>PN427and PN121>PN418).