Mutasynthesis of fluorinated pactamycin analogues and their antimalarial activity

Date

2014-4

Type

Article

Journal title

Organic Letters

Issue

Vol. 2014 No. 15

Author(s)

Khaled H Almabruk, Mostafa Abugreen, Wanli Lu, Jane X Kelly and Taifo Mahmud

Pages

1678 - 1681

Abstract

A mutasynthetic strategy has been used to generate fluorinated TM-025 and TM-026, two biosynthetically engineered pactamycin analogs 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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