Buskes Melissa J, Clements Monica, Bachovchin Kelly A, Jalani Hitesh B, Leonard Allison, Bag Seema, Klug Dana M, Singh Baljinder, Campbell Robert F, Sciotti Richard J, El-Sakkary Nelly, Caffrey Conor R, Pollastri Michael P, Ferrins Lori
Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Experimental Therapeutics, Walter Reed Army Institute of Research, 2460 Linden Lane, Silver Spring, Maryland 20910, United States.
ACS Med Chem Lett. 2020 Jan 10;11(3):258-265. doi: 10.1021/acsmedchemlett.9b00455. eCollection 2020 Mar 12.
We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, . This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
我们最近报道了一系列用于抗锥虫化合物溶解度驱动优化研究的化合物。将寄生虫跳跃方法扩展至该系列化合物，对该文库中的一部分化合物进行了针对后生动物扁虫寄生虫的交叉活性筛选。本研究报告了几种对成年血吸虫具有强效生物活性的化合物的鉴定及初步开发情况，其中一种或多种有望成为进一步评估和优化的先导化合物。
