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 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. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 5, pp. 15 – 19, May, 2005.