Synthesis of potent water-soluble tissue transglutaminase inhibitors

M Griffin, A Mongeot, R Collighan, RE Saint…

Index: Griffin, Martin; Mongeot, Alexandre; Collighan, Russell; Saint, Robert E.; Jones, Richard A.; Coutts, Ian G.C.; Rathbone, Daniel L. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5559 - 5562

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Citation Number: 61

Abstract

Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-l-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

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