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…

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

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被引用次数: 179

摘要

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 ...