Reversible and competitive cinnamoyl triazole inhibitors of tissue transglutaminase.

Abstract

A series of 15 cinnamoyl triazole derivatives was prepared by Cu(I)-catalyzed azide/alkyne [3+2]-cycloaddition reactions and examined as inhibitors of guinea-pig liver transglutaminase. Several compounds exhibited activity as reversible inhibitors that were competitive with acyl donor transglutaminase substrates. For example, triazole 4d has a K(i) value of… (More)
DOI: 10.1111/j.1747-0285.2008.00696.x

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