In-vitro and in-vivo antibacterial activities of CS-834, a new oral carbapenem.

Abstract	We evaluated the in-vitro and in-vivo antibacterial activities of R-95867 and CS-834, a new oral carbapenem which is an ester-type prodrug of R-95867. Against Gram-positive bacteria, R-95867 was as active or two to 256 times more active than cefpodoxime, cefdinir, cefditoren and ofloxacin, while its activity was similar to or two to eight times lower than that of imipenem. Against most Gram-negative bacteria it was as active or two to 1024 times more active than the other compounds tested. Against Helicobacter pylori it was two to 64 times more active than orally active anti-H. pylori agents, i.e. amoxycillin, clarithromycin and lansoprazole. It also showed potent bactericidal activity against Staphylococcus aureus and Escherichia coli. R-95867 induced a spherical form in E. coli and showed high affinity for PBP 2 in E. coli. Against systemic infections in mice caused by various bacteria, CS-834 showed an excellent protective effect and its in-vivo efficacy correlated well with the in-vitro activity of R-95867. These results suggest that CS-834 may be effective in the therapy of various bacterial infections.
Authors	E Sakagawa, M Otsuki, T Oh, T Nishino, T Ou
Journal	The Journal of antimicrobial chemotherapy (J Antimicrob Chemother) Vol. 42 Issue 4 Pg. 427-37 (Oct 1998) ISSN: 0305-7453 [Print] England
PMID	9818740 (Publication Type: Comparative Study, Journal Article)
Chemical References	Bacterial Proteins Carbapenems Carrier Proteins Penicillin-Binding Proteins Penicillins Prodrugs Peptidyl Transferases Hexosyltransferases Muramoylpentapeptide Carboxypeptidase CS 834
Topics	Administration, Oral Animals Bacteria (drug effects) Bacterial Infections (drug therapy, microbiology) Bacterial Proteins Carbapenems (metabolism, pharmacology, therapeutic use) Carrier Proteins (metabolism) Colony Count, Microbial Drug Resistance, Microbial Escherichia coli (drug effects, metabolism) Hexosyltransferases Male Mice Microbial Sensitivity Tests Microscopy, Interference Muramoylpentapeptide Carboxypeptidase (metabolism) Penicillin-Binding Proteins Penicillins (metabolism) Peptidyl Transferases Prodrugs (metabolism, pharmacology, therapeutic use) Protein Binding

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