The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
New Anti-MRSA and Anti-VRE Carbapenems; Synthesis and Structure-activity Relationships of 1β-Metyl-2-(thiazol-2-ylthio)carbapenems
MAKOTO SUNAGAWA, MASANORI ITOH, KATSUMI KUBOTA, AKIRA SASAKI, YUTAKA UEDA, PETER ANGEHRN, ANNE BOURSON, ERWIN GOETSCHI, PAUL HEBEISEN, RUDOLF L. THEN
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2002 Volume 55 Issue 8 Pages 722-757

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Abstract

Discovery of novel antimicrobial agents effective against infections caused by drugresistant 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 1β-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.

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The Journal of Antibiotics, Series A

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