Synthesis and Biological Activity of Some Mono- and Bis-ω-Ammonioalkyluracil Bromides

Compounds possessing anticholinesterase activity have been found in a series of mono- and bis-tetraalkylammonium derivatives containing uracil cycles at various distances from onium groups. These compounds are subdivided into high/moderate toxicity (in mice) and low/zero toxicity (in daphnia). Under...

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Veröffentlicht in:Pharmaceutical chemistry journal 2005-05, Vol.39 (5), p.239-244
Hauptverfasser: Zobov, V. V., Aslyamova, A. A., Berezinskii, L. A., Reznik, V. S., Akamsin, V. D., Galyametdinova, I. V., Giniyatullin, R. H., Nafikova, A. A., Latypov, Sh. K.
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Sprache:eng
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Zusammenfassung:Compounds possessing anticholinesterase activity have been found in a series of mono- and bis-tetraalkylammonium derivatives containing uracil cycles at various distances from onium groups. These compounds are subdivided into high/moderate toxicity (in mice) and low/zero toxicity (in daphnia). Under the functional loading conditions (treadmill test in mice upon i.p. drug injection), compounds with an alkylammonium chain length of n = 5 are more effective and less toxic than the reference drugs (proserine [neostigmine] and BW284c51) and induce the development of a clearly pronounced myorelaxant effect with a duration of not less than 5 days with ED sub(50) = 0.06 - 0.13 mu M/kg and LD sub(50)/ED sub(50) = 20.0 - 188.0.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-005-0125-9