Subject(s)
Muscle Contraction/drug effects , Muscle, Smooth/physiology , SRS-A/pharmacology , Animals , Arachidonic Acids/pharmacology , Dose-Response Relationship, Drug , Guinea Pigs , Ileum/physiology , Isomerism , Leukotriene B4 , Muscle, Smooth/drug effects , SRS-A/chemical synthesis , Structure-Activity Relationship , Trachea/physiologyABSTRACT
A series of 2-styryl-5-nitro-1-vinylimidazoles carrying alkylaminomethyl or amidino functions in the 4 position of the styryl ring was prepared and evaluated for antitrypanosomal activity in mice infected with Trypanosoma rhodesiense. The alkylaminomethyl compounds were found inactive against Trypanosoma cruzi infections in mice. One compound, 2-(4-methylamidinostyryl)-5-nitro-1-vinylimidazole hydrochloride, showed antitrypanosomal activity comparable to the standard drugs suramin, pentamidine, diminazene, and melarsoprol when tested ip against T. rhodesiense infected mice and also showed some activity when tested ip against T. cruzi infected mice.
Subject(s)
Nitroimidazoles/chemical synthesis , Trypanocidal Agents/chemical synthesis , Amidines/chemical synthesis , Amidines/therapeutic use , Animals , Chagas Disease/drug therapy , Mice , Nitroimidazoles/therapeutic use , Styrenes/chemical synthesis , Styrenes/therapeutic use , Trypanocidal Agents/therapeutic use , Trypanosomiasis, African/drug therapy , Vinyl Compounds/chemical synthesis , Vinyl Compounds/therapeutic useABSTRACT
A series of 33 thioacetals and hydrazones of 2-(4-formylstyryl)-5-nitro-1-vinylimidazole was prepared and examined for antitrypanosomal properties. The thioacetals were inactive as antitrypanosomal agents but three hydrazones derived from N-aminoguanidine, pyridylacethohydrazide chloride (Girard reagent P), and dimethylaminoacetohydrazide (Girard reagent D) displayed good activity against Trypanosoma rhodesiense.
