一锅法多组分合成对刚地弓形虫具有强效和选择性活性的2,3-二取代喹唑啉酮。
One-pot, multicomponent synthesis of 2,3-disubstituted quinazolin-ones with potent and selective activity against Toxoplasma gondii.
作者信息
Brown Carla E, Kong Tiffany, Bordón Claudia, Yolken Robert, Jones-Brando Lorraine, McNulty James
机构信息
Department of Chemistry and Chemical Biology, McMaster University, Hamilton, Ontario L8S 4M1, Canada.
Stanley Division of Developmental Neurovirology, Department of Pediatrics, Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287, USA.
出版信息
Bioorg Med Chem Lett. 2018 May 15;28(9):1642-1646. doi: 10.1016/j.bmcl.2018.03.036. Epub 2018 Mar 16.
The discovery of two quinazolinones with selective, single-digit micromolar activity (IC = 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.
据报道，发现了两种喹唑啉酮，它们对顶复门寄生虫刚地弓形虫的速殖子具有选择性的个位数微摩尔活性（IC = 6 - 7 μM）。这些强效且选择性的第三代衍生物在C2位含有苄氧基苄基取代基，在N3位含有一个庞大的脂肪族部分。在此，我们表明这些喹唑啉酮在已建立的感染中抑制刚地弓形虫速殖子的复制，但对速殖子侵入宿主细胞没有显著影响。
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