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Synthesis and in vitro antibacterial activity of new aminothiazole-oximepiperidone cephalosporins.

Authors :
Shen Z
Xu W
Yu J
Chen L
Zhang J
Sheng S
Dong X
Bian H
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.)

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