Article
Synthesis and biological evaluation of novel sulfonyl-naphthalene-1,4-diols as FabH inhibitors.
Bioorganic & medicinal chemistry letters - 15 Dec 2008
Alhamadsheh Mamoun M, Waters Norman C, Sachdeva Sarbjot, Lee Patricia, Reynolds Kevin A
Abstract excerpt
A series of analogs of 2-tosylnaphthalene-1,4-diol were prepared and were found to be potent 10-20 nM reversible inhibitors of the Escherichia coli FabH enzyme. The inhibitors were also effective but to a lesser degree (30 nM-5 microM), against the Mycobacterium tuberculosis and Plasmodium falciparum FabH enzymes. Preliminary SAR studies demonstrated that the sulfonyl group and naphthalene-1,4 diol were required...
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