Antiradiation compounds. 20. 1-Methylquinolinium(and pyridinium)-2-dithioacetic acid derivatives
Journal Article
·
· J. Med. Chem.; (United States)
A new class of radiation-protective compounds has been found in the bis(methylthio) and methylthio amino derivatives of 1-methylquinolinium- and 1-methylpyridinium-2-dithioacetic acids. The compounds gave good protection to mice vs. 1000-rad gamma-radiation in ip doses of 10 mg/kg or less, much lower than those required for the aminoalkyl thiols (approximately 150-600 mg/kg). The dithioacetic acid zwitterions were prepared from the base-catalyzed reaction of carbon disulfide with quinaldine and picoline methiodides, and the bis(methylthio) derivatives resulted from reaction with methyl iodide at room temperature. Replacement of one methylthio moiety took place readily on reaction of the bis(methylthio) derivatives with 1 molar equiv of an amine. The best protective activity was found with the methylthio piperidino derivative in both the quinolinium and pyridinium series.
- Research Organization:
- Massachusetts College of Pharmacy and Allied Health Sciences, Boston
- OSTI ID:
- 6935810
- Journal Information:
- J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 1; ISSN JMCMA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
560152* -- Radiation Effects on Animals-- Animals
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AMINES
AMMONIUM COMPOUNDS
ANIMALS
AROMATICS
AZAARENES
AZINES
DRUGS
ELECTROMAGNETIC RADIATION
GAMMA RADIATION
HETEROCYCLIC COMPOUNDS
IONIZING RADIATIONS
MAGNETIC RESONANCE
MAMMALS
MICE
NUCLEAR MAGNETIC RESONANCE
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
PYRIDINES
PYRIDINIUM COMPOUNDS
QUATERNARY COMPOUNDS
QUINOLINES
RADIATIONS
RADIOPROTECTIVE SUBSTANCES
RADIOSENSITIVITY EFFECTS
RESONANCE
RODENTS
VERTEBRATES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AMINES
AMMONIUM COMPOUNDS
ANIMALS
AROMATICS
AZAARENES
AZINES
DRUGS
ELECTROMAGNETIC RADIATION
GAMMA RADIATION
HETEROCYCLIC COMPOUNDS
IONIZING RADIATIONS
MAGNETIC RESONANCE
MAMMALS
MICE
NUCLEAR MAGNETIC RESONANCE
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC SULFUR COMPOUNDS
PYRIDINES
PYRIDINIUM COMPOUNDS
QUATERNARY COMPOUNDS
QUINOLINES
RADIATIONS
RADIOPROTECTIVE SUBSTANCES
RADIOSENSITIVITY EFFECTS
RESONANCE
RODENTS
VERTEBRATES