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Synthesis of functionalized 2-aryl-5-nitro-1H-indoles and their activity as bacterial NorA efflux pump inhibitors.

Abstract：

:In order to develop structure-activity relationships and to provide access to antibacterial agents for dual action studies, a variety of aryl group-substituted 2-aryl-5-nitro-1H-indoles were synthesized and the activity of the compounds assessed as inhibitors of the NorA multidrug resistance pump in the bacterium Staphylococcus aureus. The NorA protein from the major facilitator superfamily of efflux pumps confers resistance to a variety of structurally dissimilar antimicrobials such as norfloxacin, ethidium bromide, berberine and acriflavin. The compound [4-benzyloxy-2-(5-nitro-1H-2-yl)-phenyl]-methanol was the most potent pump inhibitor.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Samosorn S,Bremner JB,Ball A,Lewis K

doi

10.1016/j.bmc.2005.09.019

subject

Has Abstract

pub_date

2006-02-01 00:00:00

pages

857-65

issue

3

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00862-X

journal_volume

14

pub_type

杂志文章

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