Orally active. beta.-lactam inhibitors of human leukocyte elastase-1. Activity of 3, 3-diethyl-2-azetidinones

SK Shah, CP Dorn Jr, PE Finke, JJ Hale…

文献索引：Shah, Shrenik K.; Dorn, Conrad P.; Finke, Paul E.; Hale, Jeffrey J.; Hagmann, William K.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 21 p. 3745 - 3754

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被引用次数: 87

摘要

A thorough analysis of the mechanism of inhibition of human leukocyte elastase (HLE) by a monocyclic 8-lactam and the mechanism of@-lactam hydrolysis led to the preparation of potent and highly stable inhibitors of HLE. This work led to the identification of 4-[(4- carboxyphenyl)-oxy]-3, 3-diethyl-l-[[(phenylmethyl) aminolcarbonyl]-2-azetidinone (2) as the first orally active inhibitor of human leukocyte elastase (HLE). Analogs of 2 with different ...