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  • 1
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    Reduced immunotoxicity and preservation of antibacterial activity in a releasable side-chain carbapenem antibiotic (1999)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1999-01-29
    Description: 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.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rosen, H -- Hajdu, R -- Silver, L -- Kropp, H -- Dorso, K -- Kohler, J -- Sundelof, J G -- Huber, J -- Hammond, G G -- Jackson, J J -- Gill, C J -- Thompson, R -- Pelak, B A -- Epstein-Toney, J H -- Lankas, G -- Wilkening, R R -- Wildonger, K J -- Blizzard, T A -- DiNinno, F P -- Ratcliffe, R W -- Heck, J V -- Kozarich, J W -- Hammond, M L -- New York, N.Y. -- Science. 1999 Jan 29;283(5402):703-6.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Merck Research Laboratories, Rahway, NJ 07065, USA. hugh_rosen@merck.com〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/9924033" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Antibodies/blood ; *Bacterial Proteins ; Carbapenems/chemistry/*immunology/metabolism/*pharmacology/toxicity ; Carrier Proteins/metabolism ; Dipeptidases/metabolism ; *Drug Design ; Drug Resistance, Microbial ; Drug Resistance, Multiple ; Enterococcus/drug effects ; Erythrocytes/immunology ; Haptens ; *Hexosyltransferases ; Humans ; Immunodominant Epitopes ; Immunoglobulin G/blood ; Lactams/chemical synthesis/chemistry/metabolism/*pharmacology ; Lymphocyte Activation ; Macaca mulatta ; Mice ; Mice, Inbred DBA ; Microbial Sensitivity Tests ; Muramoylpentapeptide Carboxypeptidase/metabolism ; Penicillin-Binding Proteins ; *Peptidyl Transferases ; Staphylococcal Infections/drug therapy ; Staphylococcus/drug effects ; Thiazoles/chemical synthesis/chemistry/metabolism/*pharmacology
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 2
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    Antibacterial agents that inhibit lipid A biosynthesis (1996)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1996-11-08
    Description: Lipid A constitutes the outer monolayer of the outer membrane of Gram-negative bacteria and is essential for bacterial growth. Synthetic antibacterials were identified that inhibit the second enzyme (a unique deacetylase) of lipid A biosynthesis. The inhibitors are chiral hydroxamic acids bearing certain hydrophobic aromatic moieties. They may bind to a metal in the active site of the deacetylase. The most potent analog (with an inhibition constant of about 50 nM) displayed a minimal inhibitory concentration of about 1 microgram per milliliter against Escherichia coli, caused three logs of bacterial killing in 4 hours, and cured mice infected with a lethal intraperitoneal dose of E. coli.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Onishi, H R -- Pelak, B A -- Gerckens, L S -- Silver, L L -- Kahan, F M -- Chen, M H -- Patchett, A A -- Galloway, S M -- Hyland, S A -- Anderson, M S -- Raetz, C R -- New York, N.Y. -- Science. 1996 Nov 8;274(5289):980-2.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Department of Microbiology, Merck Research Laboratories, Rahway, NJ 07065, USA.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/8875939" target="_blank"〉PubMed〈/a〉
    Keywords: Amidohydrolases/*antagonists & inhibitors/metabolism ; Animals ; Anti-Bacterial Agents/chemistry/*pharmacology ; Binding Sites ; Escherichia coli/drug effects ; Escherichia coli Infections/drug therapy ; Gram-Negative Bacteria/*drug effects ; Hydroxamic Acids/chemistry/*pharmacology ; Lipid A/*biosynthesis ; Mice ; Microbial Sensitivity Tests ; Oxazoles/chemistry/pharmacology ; Pseudomonas/drug effects ; Serratia/drug effects ; Stereoisomerism ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
    Location Call Number Expected Availability
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