Synthesis and comparative skeletal muscle relaxant activity of some 2,4-imidazolidinediones and their corresponding 5-hydroxy-2,4-imidazolidinediones.
A series of 5-hydroxy substitution products of 2,4-imidazolidinediones, including the 5-hydroxy metabolite of the skeletal muscle contraction antagonist, dantrolene sodium, has been synthesized and evaluated for skeletal muscle relaxant activity. Most of these analogues are active in vivo with iv administration and in vitro. While two analogues are also active by oral and ip administration, only 1-[[[5-(3,4-dichlorophenyl)-2-furanyl]methylene]amino]-5-hydroxy-2,4-imidazolidinedione is sufficiently active in inhibiting the Straub tail in mice. However, none of these analogues has a muscle relaxant efficacy index greater than 1, comparable to dantrolene.
D000818:Animals; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009020:Morphine / Q000037:antagonists & inhibitors; D009119:Muscle Contraction / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis*; D004856:Postural Balance / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
D007093:Imidazoles; D009125:Muscle Relaxants, Central; D009020:Morphine