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The multiple side effects and long dosing period of current main treatment regiments calls for high effective and low toxicity anti\u2010toxoplasmosis drugs. Herein, we report our efforts to synthesize a series of 2\u2010(piperazin\u20101\u2010yl)quinazolin\u20104(3<jats:italic>H<\/jats:italic>)\u2010one derivatives and investigate their activity against <jats:italic>Toxoplasma gondii<\/jats:italic> tachyzoites in\u2005vitro based on cell phenotype screening. Among the 26 compounds, <jats:bold>8w<\/jats:bold> and <jats:bold>8x<\/jats:bold> with diaryl ether moiety at the side chain of piperazine exhibited good efficacy to inhibit <jats:italic>T. gondii<\/jats:italic>, with IC<jats:sub>50<\/jats:sub> values of 4\u2005\u03bcM and 3\u2005\u03bcM, respectively. Structure\u2010activity relationship (SAR) studies implies that hydrophobic aryl at the side chain would be preferred for improvement of activity. Molecular docking study reveals these two compounds appeared high affinity to <jats:italic>Tg<\/jats:italic>CDPK1 by interaction with the hydrophobic pocket of ATP\u2010binding cleft.<\/jats:p>","DOI":"10.1002\/cbdv.202100687","type":"journal-article","created":{"date-parts":[[2021,11,2]],"date-time":"2021-11-02T20:09:39Z","timestamp":1635883779000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["<i>In Vitro<\/i> Anti\u2010<i>Toxoplasma gondii<\/i> Activity Evaluation of a New Series of Quinazolin\u20104(3<i>H<\/i>)\u2010one Derivatives"],"prefix":"10.1002","volume":"18","author":[{"given":"Yu","family":"Deng","sequence":"first","affiliation":[{"name":"Institute of Veterinary Sciences &amp; Pharmaceuticals Chongqing Academy of Animal Sciences  51 Changlong Avenue Rongchang District 402460 China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hao","family":"Mu","sequence":"additional","affiliation":[{"name":"Institute of Veterinary Sciences &amp; Pharmaceuticals Chongqing Academy of Animal Sciences  51 Changlong Avenue Rongchang District 402460 China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5621-4409","authenticated-orcid":false,"given":"Hong\u2010Bo","family":"Li","sequence":"additional","affiliation":[{"name":"Chengdu Hyperway Pharmaceuticals Co. 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