New anti-MRSA and anti-VRE carbapenems: Synthesis and structure-activity relationships of 1β-metyl-2-(thiazol-2-ylthio)carbapenems

DOI: 10.7164/antibiotics.55.722

Source and publish data:

Journal of Antibiotics p. 722 - 757 (2002)

Update date:2022-08-03

Topics:

Authors:

Sunagawa, Makoto

Itoh, Masanori

Kubota, Kubota

Sasaki, Akira

Ueda, Yutaka

Angehrn, Peter

Bourson, Anne

Goetschi, Erwin

Hebeisen, Paul

Then, Rudolf L.

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Article abstract of DOI:10.7164/antibiotics.55.722

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 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.

Full text of DOI:10.7164/antibiotics.55.722

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