Department of Chemistry, Scripps Florida, Jupiter, Florida 33458, USA.
Org Lett. 2011 Apr 15;13(8):2034-7. doi: 10.1021/ol200420u. Epub 2011 Mar 15.
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.
淋巴丝虫病是由寄生线虫班氏吴策线虫和马来丝虫引起的,而天冬酰胺-tRNA 合成酶(AsnRS)被认为是一种极好的抗丝虫靶点。从链霉菌 17944 中发现了三种新型替兰霉素(TAMs),即 TAM E(1)、F(2)和 G(3),以及 TAM A(4)和 B(5)。值得注意的是,5 选择性抑制班氏吴策线虫的 AsnRS 并有效杀死成年班氏吴策线虫寄生虫,代表了发现和开发抗丝虫药物的新先导骨架。