Synthesis and skeletal muscle relaxant activity of 3-(aminoacyl)-1-[[[5-(substituted phenyl)-2-furanyl]methylene]amino] -2,4-imidazolidinediones.
A series of 3-(aminoacyl)-1-[[[5-(substituted phenyl)-2-furanyl] methylene]amino]-2,4-imidazolidinediones was synthesized and evaluated for skeletal muscle relaxant activity. All compounds were active by the intravenous route, and nine of 11 were active orally. One compound was very active when evaluated by the mouse Straub tail and rotarod tests; its efficacy index (ED50 rotarod/ED50 Straub tail) was 2.0, while its therapeutic index (LD50/ED50 Straub tail) was > 225.
D000818:Animals; D003620:Dantrolene / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D009132:Muscles / Q000187:drug effects; D051381:Rats
D007093:Imidazoles; D009125:Muscle Relaxants, Central; D003620:Dantrolene