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

…, AM Cantin, WA Neugebauer…

Index: Koteva; Cantin; Neugebauer; Escher Canadian Journal of Chemistry, 2001 , vol. 79, # 4 p. 377 - 387

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Citation Number: 13

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 IC50 values were obtained with neutral hydrophobic 7α-methoxy cephalosporanic acid derivatives. Tryptophanyl-9-fluorenylmethyl ester and N-benzhydryl piperazine derivatives of 7α- ...