The discovery of two quinazolinones with selective, single-digit micromolar activity (IC₅₀ = 6–7 µM) against the tachyzoites of the apicomplexan parasite Toxoplasma gondii is reported. These potent and selective third generation derivatives contain a benzyloxybenzyl substituent at C2 and a bulky aliphatic moiety at N3. Here we show that these quinazolinones inhibit T. gondii tachyzoite replication in an established infection, but do not significantly affect host cell invasion by the tachyzoites.

中文翻译：

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一锅多组分合成2,3-二取代喹唑啉酮对弓形虫具有有效的选择性活性

2个喹唑啉酮具有选择性，个位数微摩尔活性的发现（IC ₅₀ 对的顶复门寄生虫的速殖子= 6-7μM）弓形虫报道。这些有效的和选择性的第三代衍生物在C 2处含有苄氧基苄基取代基，在N 3处含有庞大的脂族部分。在这里，我们显示了这些喹唑啉酮类在已建立的感染中可抑制弓形虫速殖子的复制，但不会显着影响速殖子对宿主细胞的入侵。