Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo [2.2. 2] octane and perhydroindole derivatives

…, M Lonchampt, E Canet, G De Nanteuil

Index: Portevin, Bernard; Lonchampt, Michel; Canet, Emmanuel; De Nanteuil, Guillaume Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1906 - 1918

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Citation Number: 16

Abstract

A series of potent and selective human leukocyte elastase (HLE) inhibitors of the Val-Pro- Val type has been developed. Initially, the central proline residue was replaced by nonnatural amino acids Phi ((2 S, 3a S, 7a S)-perhydroindole-2-carboxylic acid) and Abo ((3 S)-2-azabicyclo [2.2. 2] octane-3-carboxylic acid), and secondly several groups able to confer antioxidant properties to the molecule were introduced at the lipophilic N-terminal ...