Antiradiation Drugs without Amino Groups.

摘要

Since 1 June, 1985, thirty-four novel compounds were submitted for testing of their potential for protecting animals against ionizing radiation. These included three trisulfide bissulfinates and related compounds, eleven monodisulfide monosulfinates, seven bisdisulfide bissulfinates, four analogues of WR2,721 plus three other amino disulfides, two disulfide sulfinates from convergent syntheses, and four miscellaneous compounds. Biological activities have been reported only on three of these submissions; these effected 90%, 60%, and 20% survival. Chemical studies have emphasized factors important in the synthesis and stability of the antiradiation agents submitted. In the final-year period of 1 June, 1987-30 June, 1988, one emphasis chemically has been on convergent syntheses. Two aromatic agents submitted were synthesized by such approaches, as was an intermediate designed to produced an aliphatic agent. The apparent involvement of counterparts of sulfenes in the synthesis of the aromatic agents was investigated. A second emphasis in the past year has been on the synthesis of sulfinic esters by the reactions developed with N,N'-carbonyldiimidazole and chlorotrimethylsilane. Overall, in the three-year period, 14 papers have been published or are in press, another has been submitted, and two others are in preparation. One patent application has been filed.