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U.S. Department of Energy
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Synthesis of amino derivatives of dithio acids as potential radiation-protective agents. Annual report, 15 March-31 August 1983

Technical Report ·
OSTI ID:5529062

Dithio acids should be more-effective agents for hydrogen-atom transfer to effect repair of radiation-damaged DNA or other cellular substance than thiols since the pH for maximum rate of transfer for dithio acids (pH 4-6) is closer to cellular pH for maximum rate of H transfer from thiols (pH 10-11). The synthesis of several N-methylquinolinium-2-dithioacetic acid derivatives was accomplished, and the compounds were submitted for radiation-protective screening. These included the zwitterion of the dithio acid, the bis (methylthio) derivative, and the methyl-thio N-morpholino and methylthio N-piperidino derivatives. Two of the compounds had 6-methyl substituents. Various attempts to prepare aliphatic amino dithio acid esters were made, including the reaction of an imino thio ester with H/sub 2/S, the reaction of an aledhyde with morpholine and sulfur, and the reaction of a protected thiol ester with Lawesson's reagent. None of these procedures gave pure, identifiable products.

Research Organization:
Massachusetts Coll. of Pharmacy and Allied Health Sciences, Boston (USA)
OSTI ID:
5529062
Report Number(s):
AD-A-165798/0/XAB
Country of Publication:
United States
Language:
English