Design and synthesis of 4H-3, 1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase

A Krantz, RW Spencer, TF Tam, TJ Liak…

Index: Krantz; Spencer; Tam; Liak; Copp; Thomas; Rafferty Journal of Medicinal Chemistry, 1990 , vol. 33, # 2 p. 464 - 479

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Citation Number: 179

Abstract

4H-3, 1-Benzoxazin-4-ones are alternate substrate inhibitors of the serine proteinase human leukocyte elastase (HL elastase) and form acyl enzyme intermediates during enzyme catalysis. We have synthesized a large variety of benzoxazinones using specific methods that have been adapted to achieve the pattern of ring substitution dictated by theoretical considerations. The results of the inhibition of HL elastase by 175 benzoxazinones are ...