Synstar Japan Co., Ltd., 2-9-46 Sakaecho, Odawara, Kanagawa 250-0011, Japan.
Faculty of Pharmaceutical Science, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan.
Bioorg Med Chem. 2021 Mar 1;33:116018. doi: 10.1016/j.bmc.2021.116018. Epub 2021 Jan 16.
Quinazolines have long been known to exert varied pharmacologic activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, we have synthesized approximately 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, we summarize the results and report the discovery of 6,7-dimethoxy-N-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine (20, SSJ-717), which exhibits high antimalarial activity as a promising antimalarial drug lead.
喹唑啉类化合物具有多种药理活性，长期以来一直被用于治疗高血压、病毒感染、肿瘤和疟疾。自 2014 年以来，我们已经合成了大约 150 种不同的 6,7-二甲氧基喹唑啉-2,4-二胺，并通过构效关系研究评估了它们的抗疟活性。在这里，我们总结了这些结果，并报告了发现 6,7-二甲氧基-N-(1-苯乙基)-2-(吡咯烷-1-基)喹唑啉-4-胺（20，SSJ-717），它作为一种很有前途的抗疟药物先导化合物，具有很高的抗疟活性。
