Abstract
Peptide containing phosphinic acids are peptidomimetics which have been successfidly employed m the design of inhibitors of protease and ligase enzymes. These stable tetrahedral phosphorus species act by mimicking the tetrahedral mtemediates of the reactions catalyzed by these two groups of enzymes. Using this concept potent transition-state analogue inhibitors of a wide variety of protenses, as well as of some tigases have been developed and studied m some detail. One of the key problems m the synthesis of these peptidomimetics is the conversion of readily available N-blocked 1 -aminoakylphosphonous acids or their esters mto corresponding phosphinic acids.
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