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

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.

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 ED50 = 0.06 – 0.13 µM/kg and LD50/ED50 = 20.0 – 188.0.

CHOLINESTERASE inhibitors; ENZYME inhibitors; URACIL; DRUG toxicity; DRUG interactions; MOLECULAR structure

Pharmaceutical Chemistry Journal, 2005, Vol 39, Issue 5, p239

0091-150X

Academic Journal

10.1007/s11094-005-0125-9