New anti-MRSA and anti-VRE carbapenems; synthesis and structure-activity relationships of 1beta-methyl-2-(thiazol-2-ylthio)carbapenems

Discovery of novel antimicrobial agents effective against infections caused by drug-resistant pathogens is an important objective. In order to find a new parenteral carbapenem antibiotic, which has potent antibacterial activity especially against methicillin-resistant staphylococci, vancomycin-resis...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Journal of antibiotics 2002-08, Vol.55 (8), p.722-757
Hauptverfasser:	Sunagawa, Makoto, Itoh, Masanori, Kubota, Katsumi, Sasaki, Akira, Ueda, Yutaka, Angehrn, Peter, Bourson, Anne, Goetschi, Erwin, Hebeisen, Paul, Then, Rudolf L
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Carbapenems - chemical synthesis Carbapenems - chemistry Carbapenems - pharmacology Enterococcus - drug effects Humans Methicillin Resistance Microbial Sensitivity Tests - methods Penicillin Resistance Staphylococcus aureus - drug effects Streptococcus pneumoniae - drug effects Structure-Activity Relationship Vancomycin Resistance
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Discovery of novel antimicrobial agents effective against infections caused by drug-resistant pathogens is an important objective. In order to find a new parenteral carbapenem antibiotic, which has potent antibacterial activity especially against methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant Streptococcus pneumoniae, a series of 1beta-methylcarbapenems with thiazol-2-ylthio groups at the C-2 position have been synthesized. Structure-activity relationships were investigated which led to SM-197436 (27), SM-232721 (44) and SM-232724 (41), being selected for further evaluation.
ISSN:	0021-8820