Natural product inhibitors of fatty acid biosynthesis: synthesis of the marine microbial metabolites pseudopyronines A and B and evaluation of their anti-infective activities | Academic Article individual record
abstract

Total syntheses of the title natural products, pseudopyronines A (1) and B (2), have been achieved using methyl β-oxo carboxylic ester starting materials. The natural products and a small set of structurally related compounds were evaluated for growth inhibitory activity against a range of pathogenic microorganisms and were found to exhibit good potency (IC50≥0.46 μg/mL) and selectivity towards Leishmania donovani. Several of the compounds inhibited recombinant fatty acid biosynthesis enzymes from both Plasmodium falciparum and Mycobacterium tuberculosis, validating these targets in the search for new anti-infective agents. © 2007 Elsevier Ltd. All rights reserved.

author list (cited authors)
Giddens, A. C., Nielsen, L., Boshoff, H. I., Tasdemir, D., Perozzo, R., Kaiser, M., ... Copp, B. R.
publication date
2008
publisher
Elsevier BV Publisher
published in
Tetrahedron Journal
keywords
  • Marine Natural Product
  • Leishmania
  • Mycobacteriun
  • Fatty Acid Biosynthesis
citation count

36