Subject(s)
Anticonvulsants/administration & dosage , Levodopa/administration & dosage , Parkinson Disease/drug therapy , Receptors, Cell Surface/drug effects , gamma-Aminobutyric Acid/analogs & derivatives , Clinical Trials as Topic , Double-Blind Method , Drug Synergism , Humans , Parkinson Disease/physiopathology , Receptors, GABA-A , gamma-Aminobutyric Acid/administration & dosageSubject(s)
Nervous System Diseases/metabolism , Psychotic Disorders/metabolism , Serotonin/metabolism , 5-Hydroxytryptophan/blood , 5-Hydroxytryptophan/therapeutic use , Carbidopa/therapeutic use , Female , Homovanillic Acid/cerebrospinal fluid , Humans , Hydroxyindoleacetic Acid/blood , Hydroxyindoleacetic Acid/cerebrospinal fluid , Kinetics , Middle Aged , Myoclonus/metabolism , Serotonin/bloodABSTRACT
A series of N-heterocyclic and N-heterocyclic alkyl derivatives of bis(2-aminoethyl) disulfide and aminoethanethiosulfuric acid was synthesized as potential antiradiation and anticancer agents. The compounds were prepared by the reactions of the heterocyclic halides with bis(2-aminoethyl) disulfide and aminoethanethiosulfuric acid. A dithio acid derivative, 3,3-dimercapto-2-cyanoacryloylpyrrolidide, was also prepared. Several compounds, including the dithio acid derivative, provided good radiation protection to mice. None of the compounds screened showed appreciable anticancer activities in two leukemia systems.
Subject(s)
Heterocyclic Compounds/pharmacology , Radiation Effects , Radiation-Protective Agents/pharmacology , Thiosulfates/pharmacology , Animals , Antineoplastic Agents/pharmacology , Chemical Phenomena , Chemistry , Heterocyclic Compounds/chemical synthesis , Mice , Radiation-Protective Agents/chemical synthesis , Thiosulfates/chemical synthesisABSTRACT
Based on the antimalarial activity in mice of bis(4-rho-acetamidobenzenesulfonamidophenyl) disulfide, a series of N-heterocyclic alkyl disulfides and thiosulfates was synthesized and screened for antimalarial activity. Several related dithio acid dianions and S- blocked derivatives were also screened to provide an indication of the possible role that thiol anions might play in malaria chemotherapy. Activity was limited by toxicity with these compounds, and none of those tested, with the exception of bis(4-rho-acetamidobenzenesulfonamidophenyl) disulfide, showed curative activity in either a mouse or chick test.
