Active-site-directed enzyme-activated N-nitrosoamide inhibitors of trypsin

Y Chen, EH White

Index: Chen, Yulong; White, Emil H. Organic Preparations and Procedures International, 1996 , vol. 28, # 1 p. 65 - 76

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Citation Number: 2

Abstract

This article covers the syntheses of active-site-directed enzyme-activated N-nitrosoamides (1-3), which have been found to be highly active inhibitors of trypsin.'The preparation of the N-nitroso modified amide and peptide inhibitors for trypsin posed two major problems:(1) the necessity of nitrosating an amide group in the presence of the more basic primary amino function. This problem was largely solved by keeping the amino group in its protonated ...