Synthesis of New Prophylactic Antiradiation Drugs.
Annual rept. 1 Aug 81-31 Jul 82,
ILLINOIS UNIV AT THE MEDICAL CENTER CHICAGO DEPT OF MEDICINAL CHEMISTRY
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S series of N-3-aryl-1-adamantanemethyl-alpha-mercaptoacetamidines and derivatives was synthesized. A number of 3-aryl-1-adamantanemethylamines B were synthesized first. These amines would become part of the N-substituent of the amidine function, RNH-CNH-CH2SY. The specific alpha-mercaptoacetamidines and derivatives, which were prepared, were those in which RCH3, and SY is S2O3- Bunte Salt, SPO3-2 and S-Sdisulfide ROCH3, and SY is SH,S-Sdisulfide, SPO3-2 RF, and SY is SH, S-Sdisulfide, SPO3-2 as well as RSCH3, where SY is S2O3- Bunte Salt, or SPO3-2. Of the 10 compounds sent to Walter Reed Army Institute for Research, 6 were evaluated for radiation protective potency in mice. The compounds showed some protective activity but did not show unusual promise, in part due to their relatively high toxicity.