Abstract
Some representatives of 1,3-bis-(5-ammoniopentyl)uracil dibromides with the anticholinesterase type of activity are classified as highly/moderately-toxic in mice and as slightly toxic/practically nontoxic in daphnia. Under the conditions of functional testing (treadmill running test in mice, i.p.) the compounds with less bulky substituents (H, F, Br, CH 3 , CN, NO 2 , and CH 3 O groups) at positions 5 and 6 of the uracil cycle are more effective and safe than proserin and BW284c51: (a) they induce the development of a clearly pronounced myorelaxant effect with lasting over not less than one day (ED 50 = 0.03 - 0.11 μM/kg), (b) the ratio LD 50 /ED 50 is below 76.67. An increase in length of the aliphatic radical in position 5 of the uracil cycle leads to a gradual increase in the toxicity with respect to daphnia, while the toxicity with respect to mice exhibits a decrease.
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