作者:David Rennison、Stephanie M. Gueret、Olivia Laita、Ross J. Bland、Ian A. Sutherland、Ian K. Boddy、Margaret A. Brimble
DOI:10.1071/ch16169
日期:——
modifications to lead carbazole 1 (EC100 = 2.5 μM against Haemonchus contortus in vitro), which was revealed in a small molecule screening program as a potentially promising platform for the development of new anthelmintic drugs. Subsequently, analogues 19, 21, 41, 42 (EC100 = 1.25 μM, all), and 39 (EC100 = 0.625 μM) were demonstrated to exhibit enhanced in vitro anthelmintic activity over the lead structure
基于对咔唑1的结构修饰合成了一系列新型咔唑(在体外 针对弯曲变形双链弯曲杆菌EC 100 = 2.5μM ),这在小分子筛选程序中被揭示为开发新的驱虫药的潜在前景。随后,类似物19,21,41,42(EC 100 = 1.25μM,全部),和39(EC 100 = 0.625μM)被证明在过引线结构体外驱虫活性,以表现出增强,与化合物39也被示出为在体内对Heligmosomoides聚回。