Synthesis and Myorelaxant Activity of 1,3-Bis(5-ammoniopentyl)-6-methyluracil Dihalides

A series of 1,3-bis(5-ammoniopentyl)-6-methyluracil dihalides with the anticholinesterase type of activity have been synthesized and characterized with respect to toxicity and myorelaxant activity. The obtained compounds exhibit high toxicity with respect to mice and belong to the class of low/practically zero toxicity with respect to daphnia. Under conditions of functional loading (treadmill running test) in mice, the compounds with small-volume electron-acceptor substitutes (F, NO sub(2), CN, CH sub(2) OCH sub(3), C(O)OCH sub(3) etc.) at the quaternary nitrogen atoms in the benzyl radical are more effective (upon intraperitoneal injection) and safer than the reference drugs (proserine and BW284c51) and induce the development of a clearly pronounced myorelaxant effect with a duration of no less than 1 day with ED sub(50) = 0.04 - 0.09 mu -M/kg and LD sub(50)/ED sub(50) up to 56.25.