Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines,Bioorganic & Medicinal Chemistry

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Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2021-01-16 , DOI: 10.1016/j.bmc.2021.116018
Yuki Mizukawa ₁ , Mayumi Ikegami-Kawai ₂ , Masako Horiuchi ₂ , Marcel Kaiser ₃ , Masayoshi Kojima ₁ , Seiki Sakanoue ₁ , Seiya Miyagi ₄ , Christian Nanga Chick ₄ , Hiroyuki Togashi ₁ , Masayoshi Tsubuki ₂ , Masataka Ihara ₅ , Toyonobu Usuki ₄ , Isamu Itoh ₁

Affiliation

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-N⁴-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine (20, SSJ-717), which exhibits high antimalarial activity as a promising antimalarial drug lead.

中文翻译：

寻找有效的抗疟药物先导：6,7-二甲氧基喹唑啉-2,4-二胺的合成和评价

众所周知，喹唑啉具有多种药理活性，因此适用于治疗高血压、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，我们总结了结果并报告了 6,7-二甲氧基-N ⁴ -(1-苯乙基)-2-(吡咯烷-1-基)喹唑啉-4-胺 ( 20 , SSJ-717) 的发现，其表现出高抗疟活性作为一种有前途的抗疟药物先导。

更新日期：2021-02-01

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