Reduced immunotoxicity and preservation of antibacterial activity in a releasable side-chain carbapenem antibiotic.
basic_science · Level V
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- Record sourced from PubMed, PMID 9924033.
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Abstract
A carbapenem antibiotic, L-786,392, was designed so that the side chain that provides high-affinity binding to the penicillin-binding proteins responsible for bacterial resistance was also the structural basis for ameliorating immunopathology. Expulsion of the side chain upon opening of the beta-lactam ring retained antibacterial activity while safely expelling the immunodominant epitope. L-786,392 was well tolerated in animal safety studies and had significant in vitro and in vivo activities against methicillin- and vancomycin-resistant Staphylococci and vancomycin-resistant Enterococci.
Medical subject headings
- Bacterial Proteins
- Carbapenems
- Drug Design
- Hexosyltransferases
- Lactams
- Peptidyl Transferases
- Thiazoles