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 |
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Format: | Artikel |
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. |
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ISSN: | 0091-150X 1573-9031 |
DOI: | 10.1007/s11094-005-0125-9 |