Incorporation of Trifluoromethyltriazoline in the Side Chain of 4‐Aminoquinolines: Synthesis and Evaluation as Antiplasmodial Agents
作者:Kanchan Yadav、Anamika Sharma、Salique Hassan Shaham、Sanoop P Chandrasekharan、Sandeep Kumar、Anamika Dhami、Hisana Nasreen、Kishor Mohanan、Renu Tripathi
DOI:10.1002/cmdc.202200653
日期:——
We identified a novel class of 4-aminoquinoline-trifluormethyltriazolines as potential antiplasmodial agents. The compounds were accessed through a silver-catalyzed three-component reaction of trifluorodiazoethane with in situ generated Schiff base from corresponding quinolinylamine and aldehydes. Four of the 32 compounds showed promising antimalarial activity: IC50 values 4–20 nM against Pf3D7 (c
我们确定了一类新的 4-氨基喹啉-三氟甲基三唑啉作为潜在的抗疟原虫药物。这些化合物是通过银催化的三氟二氮乙烷与相应的喹啉胺和醛原位生成的席夫碱的三组分反应获得的。32 种化合物中的四种显示出有前途的抗疟活性:针对 Pf3D7(氯喹敏感)的IC 50值为 4-20 nM,针对 PfK1(氯喹抗性)菌株为 120-450 nM。一种化合物在动物研究中也有效,感染后第 7 天寄生虫负荷减少 99.9%,治愈率达到 40%,宿主寿命最长。