Antiradiation Drugs Without Amino Groups.

摘要

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 RSS(CH2)4SO2Na. Other types submitted included a cyclic thiosulfinate, three bisdisulfides containing 2-aminoethyl groups and three bisdisulfides containing 2-(3-aminopropyl)aminoethyl 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.