New anti-MRSA and anti-VRE carbapenems ; Synthesis and structure-activity relationships of 1 beta-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...

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Published inJournal of antibiotics Vol. 55; no. 8; pp. 722 - 757
Main Authors Sunagawa, M, Itoh, M, Kubota, K, Sasaki, A, Ueda, Y, Angehrn, P, Bourson, A, Goetschi, E, Hebeisen, P, Then, RL
Format Journal Article
LanguageEnglish
Published TOKYO JAPAN ANTIBIOT RES ASSN 01.08.2002
Subjects
Biotechnology & Applied Microbiology
Immunology
Life Sciences & Biomedicine
Microbiology
Pharmacology & Pharmacy
Science & Technology
INFECTIONS
ANTIBIOTICS
SERIES
ANTIBACTERIAL ACTIVITY
ENTEROCOCCUS-FAECIUM
QUINUPRISTIN/DALFOPRISTIN
PART 1
CEPHALOSPORINS
RESISTANT STAPHYLOCOCCUS-AUREUS
DERIVATIVES
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Summary: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-yithio 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
DOI:10.7164/antibiotics.55.722