Synthesis and evaluation of novel β-lactam inhibitors of human leukocyte elastase-Reference-Cited by-同舟云学术

Synthesis and evaluation of novel β-lactam inhibitors of human leukocyte elastase

Published:2001-04-01 Issue:4 Volume:79 Page:377-387
ISSN:0008-4042
Container-title:Canadian Journal of Chemistry
language:en
Short-container-title:Can. J. Chem.

Author:

Koteva K P,Cantin André M,Neugebauer W A,Escher E

Abstract

A series of β-lactam derivatives were synthesized and tested to determine the structure-activity relationship for inhibition of human leukocyte elastase (HLE), a serine protease involved in several degenerative lung and tissue diseases. The most potent IC50values were obtained with neutral hydrophobic 7α-methoxy cephalosporanic acid derivatives. Tryptophanyl-9-fluorenylmethyl ester and N-benzhydryl piperazine derivatives of 7α-methoxy cephalosporanic acid represent two novel HLE inhibitors, with length of action persisting beyond 24 h.Key words: β-lactams, neutrophil elastase, protease inhibitors, peptides.

Publisher

Canadian Science Publishing

Subject

Organic Chemistry,General Chemistry,Catalysis

Link

http://www.nrcresearchpress.com/doi/pdf/10.1139/v01-062

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