Mutasynthesis of Fluorinated Pactamycin Analogues and Their Antimalarial Activity

被引:35
作者
Almabruk, Khaled H. [1 ]
Lu, Wanli [1 ]
Li, Yuexin [2 ]
Abugreen, Mostafa [1 ]
Kelly, Jane X. [2 ]
Mahmud, Taifo [1 ]
机构
[1] Oregon State Univ, Dept Pharmaceut Sci, Corvallis, OR 97331 USA
[2] Vet Affairs Med Ctr, Portland, OR 97239 USA
关键词
STREPTOMYCES-PACTUM; BIOSYNTHESIS;
D O I
10.1021/ol4004614
中图分类号
O62 [有机化学];
学科分类号
070303 [有机化学];
摘要
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.
引用
收藏
页码:1678 / 1681
页数:4
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