Anthelmintic macrolactams from Nonomuraea turkmeniaca MA7364

被引:18
作者
Ayers, Sloan
Zink, Deborah L.
Mohn, Kenneth
Powell, Joanne Staats
Brown, Christine M.
Murphy, Terry
Grund, Alan
Genilloud, Olga
Salazar, Oscar
Thompson, Donald
Singh, Sheo B.
机构
[1] Merck Res Labs, Nat Prod Chem, Rahway, NJ 07065 USA
[2] Merck & Co Inc, Branchburg Farm, Somerville, NJ 08876 USA
[3] BioTech Resources, Manitowoc, WI 54220 USA
[4] Merck Sharp & Dohme Espana SA, Ctr Invest Basica, Madrid 28027, Spain
来源
JOURNAL OF NATURAL PRODUCTS | 2007年 / 70卷 / 08期
关键词
D O I
10.1021/np070131e
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Two new macrolactams, 6-desmethyl-N-methylfluvirucin A(1) (1) and N-methylfluvirucin A(1) (2), have been isolated from the acetone extract of Nonomuraea turkmeniaca MA7364. These compounds were isolated by bioassay-guided fractionation as part of our search for new anthelmintics. The structures of these compounds were elucidated by comparison of their NMR and MS data to those of previously reported fluvirucins and confirmed by 2D NMR. Compound 1 exhibited in vitro activity (EC90 15 +/- 5 mu g/mL) against Haemonchus contortus larvae, whereas compound 2, while a bit less active in vitro (EC90 29 +/- 8 mu g/mL), showed modest in vivo activity against a surrogate organism, Heligmosomoides polygyrus in mice, at 50 mg/kg.
引用
收藏
页码:1371 / 1373
页数:3
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