Ayers Sloan, Zink Deborah L, Powell Joanne Staats, Brown Christine M, Grund Alan, Genilloud Olga, Salazar Oscar, Thompson Donald, Singh Sheo B
Natural Products Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
J Antibiot (Tokyo). 2008 Feb;61(2):59-62. doi: 10.1038/ja.2008.110.
A new macrolactam, fluvirucin B0 (1), and two known macrolactams, Sch 38516/fluvirucin B1 (2) and Sch 39185/fluvirucin B3 (3), have been isolated from an acetone extract of a strain of Nonomuraea turkmeniaca. 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. 1approximately 3 exhibited in vitro activity (EC90 <1.0 approximately 1.7 microg/ml) against Haemonchus contortus larvae, but were ineffective in reducing worm counts in vivo against Heligmosomoides polygyrus in mice at 50 mg/kg dosed intramuscularly.
从土库曼诺卡氏菌菌株的丙酮提取物中分离出一种新的大环内酯类化合物氟维菌素B0（1）以及两种已知的大环内酯类化合物Sch 38516/氟维菌素B1（2）和Sch 39185/氟维菌素B3（3）。作为我们寻找新型驱虫药工作的一部分，这些化合物是通过生物活性导向分级分离法分离得到的。通过将它们的核磁共振（NMR）和质谱（MS）数据与先前报道的氟维菌素的数据进行比较，阐明了这些化合物的结构，并通过二维核磁共振（2D-NMR）得到证实。化合物1至3对捻转血矛线虫幼虫表现出体外活性（EC90＜1.0至1.7微克/毫升），但以50毫克/千克的剂量肌肉注射时，在体内对小鼠体内的多毛螺旋线虫减少虫数方面无效。
