4.8 Article

Mutasynthesis of Fluorinated Pactamycin Analogues and Their Antimalarial Activity

Journal

ORGANIC LETTERS
Volume 15, Issue 7, Pages 1678-1681

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol4004614

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Funding

  1. OSU College of Pharmacy
  2. Environmental Health Sciences Center, Oregon State University, National Institute of Environmental Health Sciences, NIH [P30 ES00210]

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A mutasynthetic strategy has been used to generate fluorinated TM-025 and TM-026, two biosynthetically engineered pactamycin analogues produced by Streptomyces pactum ATCC 27456. The fluorinated compounds maintain excellent activity and selectivity toward chloroquine-sensitive and multidrug-resistant strains of malarial parasites as the parent compounds. The results also provide insights into the biosynthesis of 3-aminobenzoic acid in S. pactum.

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