ABSTRACT
Toxicity and radioprotective properties of 17 chemical compounds containing a hydrazine fragment have been studied in experiments on mice. It has been established that the radioprotective action of the test compounds does not depend substantially on whether the hydrazine fragment enters the heterocyclic moiety fully, partly or as an exocyclic substituent in the ring.
Subject(s)
Heterocyclic Compounds/toxicity , Hydrazines/toxicity , Radiation-Protective Agents , Animals , Dose-Response Relationship, Drug , Female , Guinea Pigs , Heterocyclic Compounds/therapeutic use , Hydrazines/therapeutic use , Lethal Dose 50 , Radiation Injuries, Experimental/prevention & control , Structure-Activity RelationshipABSTRACT
Acute toxicity and radioprotective properties of 16 derivatives of tetrahydro- and dihydropyrimidines were studied in experiments on mice. Hydroiodides of 4,6,6-trimethyl-3,R-2-methylthio-3,6-dihydropyrimidines were shown to be more toxic than respective hydroiodides of 4,6,6-trimethyl-3-R-2-methylthio-4-oxy-3,4,5,6-tetrahydropyrimidines. Four compounds exhibited moderate radioprotective properties.
Subject(s)
Pyrimidines/toxicity , Radiation-Protective Agents , Animals , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Female , Gamma Rays , Lethal Dose 50 , Mice , Radiation Dosage , Structure-Activity Relationship , Time FactorsABSTRACT
Toxicity and radioprotective properties of 18 derivatives of oxazine and thiazine with a varying degree of the cycle saturation were studied in experiments on mice. Monotypic regularity in variations of their toxic properties relative to the chemical structure was noted. 4,4,6-Trimethyl-2-dimethylamino-4H-1,3-oxazine exerted a pronounced radioprotective action.
Subject(s)
Oxazines/toxicity , Radiation-Protective Agents , Thiazines/toxicity , Animals , Gamma Rays , Injections, Intraperitoneal , Lethal Dose 50 , Male , Mice , Structure-Activity RelationshipABSTRACT
Toxicity, radioprotective and antiinflammatory properties of 20 vinyl derivatives of quinoline and products of their transformations were studied in experiments on Wistar mice and rats. The salts of quinoline vinyl derivatives (compounds VI, IX, XII, and XVIII) were shown to be more toxic than respective initial compounds (VI, VIII, XI and XVI). 8-(beta-Butylthio)-ethyloxyquinoline (compound IV) protected 25% of irradiated mice from death. Compounds I, XII, XVI and XVIII exerted a radioprotective action (in 10-15%), whereas the remaining substances proved ineffective. The combination of 8-vinyloxyquinoline and iodine (compound IV) elicited a marked antiinflammatory action in experimental serotonin-, dextran- and to a less measure formalin-induced inflammation.
Subject(s)
Quinolines/pharmacology , Vinyl Compounds/pharmacology , Animals , Anti-Inflammatory Agents , Female , Lethal Dose 50 , Mice , Quinolines/toxicity , Radiation-Protective Agents , Vinyl Compounds/toxicityABSTRACT
Test on mice demonstrated the radio-protective activity of 12 derivatives of 4-oxyhexahydropyrimidinethione-2 and 1,2,3,6-tetrahydropyrimidinethione-2 well-marked with intraperitoneal administration 10--20 minutes prior to irradiation (1000 r, exposure dose rate--10 r/min). As a whole the tetrahydroderivates are more toxic.
Subject(s)
Pyrimidinones/pharmacology , Radiation-Protective Agents , Animals , Gamma Rays/adverse effects , Lethal Dose 50 , Mice , Pyrimidinones/toxicitySubject(s)
Isothiuronium/analogs & derivatives , Organophosphorus Compounds/pharmacology , Radiation-Protective Agents/pharmacology , Thiourea/analogs & derivatives , Animals , Cystamine/pharmacology , Dose-Response Relationship, Drug , Gamma Rays , Isothiuronium/pharmacology , Isothiuronium/toxicity , Lethal Dose 50 , Male , Mice , Organophosphorus Compounds/toxicity , Radiation Injuries, Experimental/drug therapy , Radiation-Protective Agents/toxicity , Structure-Activity RelationshipABSTRACT
In experiments set up on mice, rats and guinea pigs 8 gamma-pyron derivatives were studied. They proved to be little toxic, do not change significantly the arterial pressure and respiration, exercise a depressing action on the central nervous system, produce a marked antiphlogistic (normal and irradiated animals), radio-protective and antihistaminic effects and influence norephinephrine, homovanillic acid and dopamine metabolism in the brain.