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Design, synthesis and biological evaluation of monobactams as antibacterial agents against gram-negative bacteria.

Abstract：

:A series of monobactam derivatives were prepared and evaluated for their antibacterial activities against susceptible and resistant Gram-negative strains, taking Aztreonam and BAL30072 as the leads. Six conjugates (12a-f) bearing PIH-like siderophore moieties were created to enhance the bactericidal activities against Gram-negative bacteria based on Trojan Horse strategy, and all of them displayed potencies against susceptible Gram-negative strains with MIC ≤ 8 μg/mL. SAR revealed that the polar substituents on the oxime side chain were beneficial for activities against resistant Gram-negative bacteria. Compounds 19c and 33a-b exhibited the promising potencies against ESBLs-producing E. coli and Klebsiella pneumoniae with MICs ranging from 2 μg/mL to 8 μg/mL. These results offered powerful information for further strategic optimization in search of the antibacterial candidates against MDR Gram-negative bacteria.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Fu HG,Hu XX,Li CR,Li YH,Wang YX,Jiang JD,Bi CW,Tang S,You XF,Song DQ

doi

10.1016/j.ejmech.2016.01.024

subject

Has Abstract

pub_date

2016-03-03 00:00:00

pages

151-63

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30025-3

journal_volume

110

pub_type

杂志文章

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