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Synthesis and in vitro antibacterial activity of new aminothiazole-oximepiperidone cephalosporins.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 May 15; Vol. 40, pp. 127928. Date of Electronic Publication: 2021 Mar 08. - Publication Year :
- 2021
-
Abstract
- Four new aminothiazole-oximepiperidone cephalosporins (10a-10d) were synthesized, with their in vitro antibacterial activities against hospital isolated Gram-negative bacteria assessed. The results showed that compounds 10a-10d effectively inhibit a variety of Gram-negative bacteria. Compound 10a was the most potent compound, with comparable activity as ceftazidime. The combination of compound 10a and Avibactam was very active against almost all bacteria tested, which including multidrug resistant K. pneumoniae and A. baumannii. Compared to Avycaz, this combination is more potent against ESBL producing K. pneumoniae. Thus, the combination of 10a and Avibactam is of interest for further studies.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Azabicyclo Compounds pharmacology
Cephalosporins chemical synthesis
Drug Combinations
Gram-Negative Bacteria drug effects
Microbial Sensitivity Tests
Oximes chemical synthesis
Piperidones chemical synthesis
Thiazoles chemical synthesis
Anti-Bacterial Agents pharmacology
Cephalosporins pharmacology
Oximes pharmacology
Piperidones pharmacology
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 40
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 33705899
- Full Text :
- https://doi.org/10.1016/j.bmcl.2021.127928