Reaction of COTC with Glutathione: Structure of the Putative Glyoxalase I Inhibitor

Abstract
The structure of the active glyoxalase I inhibitor derived from the Streptomyces griseosporeus metabolite COTC 1 has been conclusively identified by means of total synthesis as 2c. Human glyoxalase I is competitively inhibited by 2c (Ki = 183 ± 6 μM) but is not inhibited by 1 itself.