Antiradiation Drugs Without Amino Groups.
Annual summary rept. 1 Jun 86-31 May 87,
VANDERBILT UNIV NASHVILLE TN DEPT OF CHEMISTRY
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In the synthesis of novel antiradiation agents, 14 submissions have been made for biological testing. These included 7 representative 4-butanesulfinates terminated by a variety of Polar, non-polar, and sulfur-containing functions to give the general formulation of RSSCH24SO2Na. Other types submitted included a cyclic thiosulfinate, three bisdisulfides containing 2-aminoethyl groups and three bisdisulfides containing 2-3-aminopropylaminoethyl groups. These 14 compounds should provide good insight as to radioprotective properties of the classes they typify. Studies still in progress are reported on efforts to develop crystalline esters of sulfinic acids that will be more easily purified and more stable than their radioprotective parents. Other studies are continuing on convergent syntheses in which disulfides are to be coupled with sulfinate functions by ester linkages. No biological results have been received as yet on any of the foregoing compounds. Numerous aspects are reported of the chemistry of the compounds involved. Seven papers have been published and two others have been submitted one patent application has been filed. Keywords Acids Esters Sulfinic acids Sulfur compounds.