Halogenated 1-(4-aminobenzylidene)indenes.
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The effects of ten 1-substituted 2-n-butyl-5,6-methylenedioxyindenes on mice and guinea pigs were investigated for their allergic reactions in the development of a new anti-allergic drug. Anti-allergic effects were determined by testing the effect of agents on passive cutaneous anaphylaxis (PCA) in mice and Schultz-Dale reaction in guinea pig tracheal muscle. 2-Butyl-1-[N-methyl-N-[2-(N',N'-dimethylamino) ethyl]amino]5,6- methylenedioxyindene (1) indicated the most potent anti-allergic activity. Since our previous experiments indicated that 2-n-butyl 3-dimethyl amino-5,6-methylenedioxyindene (MDI-A) and its derivatives showed a potent anti-allergic effect by interfering with the calcium (Ca) movement in the allergic reaction in guinea pigs, the effect of 1 and MDI-A on allergic reaction and Ca-induced contraction of tracheal muscle in these animals were compared. The present data indicate the superiority of 1 in both reactions.
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