二氨基嗪乙酸酯 (DA)、二丙酸亚胺卡 (ID)、阿托伐醌 (ATO)、阿奇霉素 (AZI)、克林霉素和奎宁多年来一直用于治疗动物和人类巴贝西虫病，尽管它们有负面影响且耐药迹象不断增加。因此，寻找可以治疗感染或降低药物剂量的抗巴贝虫化合物一直是首要目标。喹唑啉是最重要的氮杂环化合物之一，具有广泛的药理活性，包括镇痛、抗炎、镇静催眠、抗组胺、抗癌和抗原虫特性。本研究调查了 20 种 6,7-二甲氧基喹唑啉-2,4-二胺对巴贝虫属的抗巴贝虫活性。一种候选药物 6,7-二甲氧基-N4-乙基异丙基-N2-乙基(吡啶-4-基)喹唑啉-2,4-二胺 (SHG02) 在体外对吉布氏巴贝虫以及田鼠巴贝虫表现出有效的抑制作用和 B. rodhaini 在小鼠中。我们的研究结果表明，候选化合物 SHG02 有望进一步开发抗巴贝虫药物，并为开发抗巴贝虫疗法提供了新的结构。版权所有 © 2023。由 Elsevier B.V. 出版。

Diminazene aceturate (DA), imidocarb dipropionate (ID), atovaquone (ATO), azithromycin (AZI), clindamycin, and quinine have been used to treat animal and human babesiosis for many years, despite their negative effects and rising indications of resistance. Thus, finding anti-babesial compounds that can either treat the infection or lower the dose of drugs given has been a primary objective. Quinazolines are one of the most important nitrogen heterocycles, with a wide range of pharmacological activities including analgesic, anti-inflammatory, sedative-hypnotic, anti-histaminic, anti-cancer, and anti-protozoan properties. The present study investigated the anti-babesial activities of twenty 6,7-dimethoxyquinazoline-2,4-diamines on Babesia spp. One candidate, 6,7-dimethoxy-N4-ethylisopropyl-N2-ethyl(pyridin-4-yl)quinazoline-2,4-diamine (SHG02), showed potent inhibition on Babesia gibsoni in vitro, as well as on B. microti and B. rodhaini in mice. Our findings indicate that the candidate compound SHG02 is promising for further development of anti-babesial drugs and provides a new structure to be explored for developing anti-Babesia therapeutics.Copyright © 2023. Published by Elsevier B.V.