支架与寄生物转移：新型原生动物增殖抑制剂的发现
Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.
作者信息
Singh Baljinder, Bernatchez Jean A, McCall Laura-Isobel, Calvet Claudia M, Ackermann Jasmin, Souza Julia M, Thomas Diane, Silva Everton M, Bachovchin Kelly A, Klug Dana M, Jalani Hitesh B, Bag Seema, Buskes Melissa J, Leed Susan E, Roncal Norma E, Penn Erica C, Erath Jessey, Rodriguez Ana, Sciotti Richard J, Campbell Robert F, McKerrow James, Siqueira-Neto Jair L, Ferrins Lori, Pollastri Michael P
机构信息
Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
出版信息
ACS Med Chem Lett. 2020 Jan 10;11(3):249-257. doi: 10.1021/acsmedchemlett.9b00453. eCollection 2020 Mar 12.
Abstract
Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against , plus 31 new compounds, against a variety of protozoan parasites including , , and . This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.
摘要
利用靶点重新利用和宿主转换方法，我们测试了一个先前报道的对[未提及的某种物质]有活性的化合物库以及31种新化合物，用于对抗多种原生动物寄生虫，包括[未提及的三种寄生虫名称]。这导致发现了几种具有亚微摩尔活性且理化性质有所改善的化合物，这些化合物是开发针对动基体疾病和疟疾的化疗药物的早期先导物。
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