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Accession Number:
ADB100049
Title:
Synthesis of amino Derivatives of Dithio Acids as Potential Radiation Protective Agents
Descriptive Note:
Annual rept. 1 Sep 1983-31 Aug 1984
Corporate Author:
MASSACHUSETTS COLL OF PHARMACY AND ALLIED HEALTH SCIENCES BOSTON
Report Date:
1984-08-01
Pagination or Media Count:
22.0
Abstract:
Appreciable radiation-protective properties were found with the N- methyl-quinolinium-2-dithioacetic acid derivatives. The bisthiomethyl and thio-methyl amino derivatives gave much greater protection 60-70 survival vs. 1000 rads than the dithio acid zwitterion 20 survival, however. These derivatives were active at much lower dosage levels 2-10 mgkg than either the dithio acid zwitterion 75 mgkg or the amino thiols 150-600 mgkg. To improve stability and distribution properties of these derivatives, inclusion of hydroxy and alkoxy functions, additional amino functions, and longer aliphatic chains in the amine portion of the methylthio amino derivatives was carried out. Also, the preparation of the corresponding N-methyl-picoline derivatives was accomplished. Use of N-methyl-2,6-dimethylpyridine also allowed the synthesis of a bisdithioacetic acid function not obtainable in the quinoline series. Several aminocyclopentenedithio acids were prepared, and the reaction of 1,2- dithiole-3-thiones with amines was carried out, giving 3-amino-2- phenyldithiopropenoate esters. Stable copper II complexes of the N- methylquinolinium-2-bismethylthio-vinyl and methylthio amino compounds were prepared and characterized. Since the bismethylthio and methylthio amino derivatives were radiation-protective at a much lower dose level than the amino thiols and have no transferable H atoms, it is probable that they are active by a different mechanism than that of the amino thiols.
Distribution Statement:
APPROVED FOR PUBLIC RELEASE
