A new group of 1- and 7-[[omega]-(benzhydryl-1-alkyl]-3-methylxanthine derivatives with antihistamine activity

Directed synthesis using the accessible compound 3-methylxanthine was used to obtain a new group of 1- and 7-[[omega]-(benzhydryl-1)alkyl]-3-methylxanthrne derivatives which functioned as histamine receptor blockers. The compound which was most active, had the longest duration of action, and the low...

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Veröffentlicht in:Pharmaceutical chemistry journal 2011-04, Vol.45 (1), p.1
Hauptverfasser: Glushkov, R.G, Yuzhakov, S.D, Alekseev, M.V, Fominova, O.S, Shorr, V.A, Zhdanov, G.F, Dolginova, E.M, Sazonova, N.M, Andreeva, N.I, Salin, E.N, Asnina, V.V
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Sprache:eng
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Zusammenfassung:Directed synthesis using the accessible compound 3-methylxanthine was used to obtain a new group of 1- and 7-[[omega]-(benzhydryl-1)alkyl]-3-methylxanthrne derivatives which functioned as histamine receptor blockers. The compound which was most active, had the longest duration of action, and the lowest toxicity was 7-[4-(4-benzhydrylpiperazinyl-1)butyl]-3-methylxanthine succinate, and this compound was selected for clinical trials. Key words: 1- and 7-[[omega]-(benzhydryl-1)alkyl]-3-methylxanthrne derivatives, synthesis, antihistamine activity, acute toxicity, further pharmacological study of 7-[4-(4-benzhydrylpiperazinyl-1)butyl]-3-methylxanthine succinate.
ISSN:0091-150X