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Synthesis, antimicrobial activity and possible mechanism of action of 9-bromo-substituted indolizinoquinoline-5,12-dione derivatives.

Abstract：

:A series of 9-bromo-substituted indolizinoquinoline-5,12-dione derivatives was synthesized. Antimicrobial activity assessment indicates that compounds 1, 26, 27 and 28 exhibit strong activity against gram-positive bacterial strains, including Beta-hemolytic streptococcus CMCC32210, Staphylococcus aureus ATCC25923, Staphylococcus epidermidis ATCC12228, Enterococcus faecalis ATCC29212 and methicillin-resistant S. aureus ATCC43300 (MRSA). Compound 27 shows the best anti-MRSA activity with an MIC value of 0.031 μg/ml. To assess the mechanism of action, the inhibitory activities of compound 1 against DNA gyrase and DNA topoisomerase IV were also measured. The results indicate that compound 1 has strong inhibitory effects on the Escherichia coli DNA gyrase supercoiling activity and S. aureus Topo IV relaxing activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wu XW,Wu ZP,Wang LX,Zhang HB,Chen JW,Zhang W,Gu LQ,Huang ZS,An LK

doi

10.1016/j.ejmech.2011.07.042

subject

Has Abstract

pub_date

2011-09-01 00:00:00

pages

4625-33

issue

9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00555-1

journal_volume

46

pub_type

杂志文章

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