Giddens, Anna C.2; Nielsen, Lone9; Boshoff, Helena I.4; Tasdemir, Deniz5; Perozzo, Remo6; Kaiser, Marcel7; Wang, Feng8; Sacchettini, James C.8; Copp, Brent R.2
1 Department of Chemistry, Faculty of Science, Aarhus University, Aarhus University2 The University of Auckland3 iNano-School, Science and Technology, Aarhus University4 NIH5 University of London6 University of Geneva7 Swiss Tropical Institute8 Texas A&M University9 iNano-School, Science and Technology, Aarhus University
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.