Journal of Medicinal Chemistry · 1986 · 34 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryStructure-activity RelationshipsSynthetic Medicinal ChemistryAmino Acid ChemistryMolecular Mechanisms Of ToxicityRadiopharmaceutical DesignRadiopharmaceuticalsStructure-activity Relationship AnalysisChemical Structure-activity RelationshipsCysteamine TherapyN-acetylcysteine PharmacologyPurine ChemistryRadioprotective AgentsRadioprotective EffectsRadioprotective Mechanisms
A variety of N-(aminoalkanoyl)-S-acylcysteamine and N,N'-bis(aminoalkanoyl)cystamine salt derivatives were synthesized. Toxicity and radioprotective activity (as the dose reduction factor DRF) were determined in vivo on mice and compared to WR 2721 and S-acetylcysteamine hydrochloride. One of the most interesting compounds of this series was N-glycyl-S-acetylcysteamine trifluoroacetate (16, I 102). Structure-activity relationships are discussed.