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Org Lett. 2011 Apr 15;13(8):2034-7. doi: 10.1021/ol200420u. Epub 2011 Mar 15.

Tirandamycins from Streptomyces sp. 17944 inhibiting the parasite Brugia malayi asparagine tRNA synthetase.

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1
Department of Chemistry, Scripps Florida, Jupiter, Florida 33458, USA.

Abstract

Lymphatic filariasis is caused by the parasitic nematodes Brugia malayi and Wuchereria bancrofti, and asparaginyl-tRNA synthetase (AsnRS) is considered an excellent antifilarial target. The discovery of three new tirandamycins (TAMs), TAM E (1), F (2), and G (3), along with TAM A (4) and B (5), from Streptomyces sp. 17944 was reported. Remarkably, 5 selectively inhibits the B. malayi AsnRS and efficiently kills the adult B. malayi parasite, representing a new lead scaffold to discover and develop antifilarial drugs.

PMID:
21405052
PMCID:
PMC3074013
DOI:
10.1021/ol200420u
[Indexed for MEDLINE]
Free PMC Article
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