Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 4, Pages 879-883Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.11.067
Keywords
FabH; fatty acid biosynthesis; inhibition; SAR; antimalarial
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Funding
- NIAID NIH HHS [AI52230] Funding Source: Medline
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A series of cyclic sulfones has been synthesized and their activity against beta-ketoacyl-ACP-synthase III (FabH) has been investigated. The compounds are selectively active against Escherichia coli FabH (ecFabH), but not Mycobacterium tuberculosis FabH (mtFabH) or Plasmodium falciparum KASIII (PfKASIII). The activity against ecFabH ranges from 0.9 to > 100 mu M and follows a consistent general SAR trend. Many of the compounds were shown to have antimalarial activity against chloroquine (CQ)sensitive (D6) P. falciparaan (IC50 = 5.3 mu M for the most potent inhibitor) and some were active against E coli (MIC = 6.6 mu g/ml for the most potent inhibitor). (c) 2006 Elsevier Ltd. All rights reserved.
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