鼻病毒
化学
细胞毒性
结构-活动关系
嘧啶
立体化学
药物发现
小分子
生物化学
体外
病毒学
病毒
生物
作者
Prashant Chakrasali,Dasom Hwang,Joo‐Youn Lee,Eunhye Jung,Hye Lim Lee,Alba Reneesh,Adam Skarka,Kamil Musílek,Nhung Hong Nguyen,Jin Soo Shin,Young‐Sik Jung
标识
DOI:10.1016/j.ejmech.2024.116690
摘要
Small molecules that exhibit broad-spectrum enteroviral inhibitory activity by targeting viral replication proteins are highly desired in antiviral drug discovery studies. To discover new human rhinovirus (hRV) inhibitors, we performed a high-throughput screening of 100,000 compounds from the Korea Chemical Bank library. This search led to identification of two phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) inhibitors having the pyrazolo-pyrimidine core structure, which display moderate anti-rhinoviral activity along with mild cytotoxicity. The results of a study aimed at optimizing the activity of the hit compounds showed that the pyrazolo-pyrimidine derivative 6f exhibits the highest activity (EC
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