Novel, Orally Effective Cyanide Antidotes

J. Med. Chem., 50 (26), 6462–6464 10.1021/jm7011497
Web Release Date: November 27, 2007

Novel, Orally Effective Cyanide Antidotes

Herbert T. Nagasawa,^*^†^‡ David J. W. Goon,^†^‡ Daune L. Crankshaw,^†^‡ Robert Vince,^† and Steven E. Patterson^†

Center for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, Minnesota 55455, and Medical Research Laboratories, DVA Medical Center, Minneapolis, Minnesota 55417

Received September 13, 2007

Abstract:

A series of prodrugs of 3-mercaptopyruvate (3-MP), the substrate for the enzyme 3-mercaptopyruvate/cyanide sulfurtransferase (3-MPST) that converts cyanide to the nontoxic thiocyanate, which are highly effective cyanide antidotes, have been developed. These prodrugs of 3-MP are unique in being not only orally bioavailable, but may be administered up to an hour prior to cyanide as a prophylactic agent and are both rapid- or slow-acting when given parenterally.

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