Inhibition of human leukocyte elastase. 6. Inhibition by 6-substituted penicillin esters

Autor: Shrenik K. Shah, Pam S. Dellea, Paul E. Finke, James B. Doherty, Kevan R. Thompson, Karen M. Hand, D. S. Fletcher, Alan L. Maycock, Bonnie M. Ashe, Mary Ellen Dahlgren
Rok vydání: 1993
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 3:2283-2288
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(01)80940-9
Popis: Penicillin amides substituted at C-6 with either an α- or β-trifluoroacetamido or an α-alkoxy functionality are reported as human leukocyte elastase (HLE) inhibitors. The structure activity relations for these derivatives are discussed and compared to the corresponding known cephalosporin structures in terms of chemical stability, HLE inhibition, and efficacy in an intratracheal (IT) lung hemorrhage assay.
Databáze: OpenAIRE