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A reassessment of mycophenolic acid as a lead compound for the development of inhibitors of chikungunya virus replication
Tetrahedron ( IF 2.1 ) Pub Date : 2017-12-28 , DOI: 10.1016/j.tet.2017.12.053
Adel A. Rashad , Johan Neyts , Pieter Leyssen , Paul A. Keller

Mycophenolic acid (MPA) has been previously reported as an inhibitor of the chikugunya virus (CHIKV) with an EC50 value of 0.2 μM. We used MPA as a lead compound designing and synthesizing a series of isatins and benzolactones in a typical medicinal chemistry program. The synthesis and testing of 19 derivatives produced compounds with no desired activity which prompted us to retest the lead compound, MPA. We can reveal that MPA shows no anti-CHIKV activity and therefore needs to be reassessed as a lead compound for this target.



中文翻译:

作为主要化合物的麦考酚酸的重新评估,以开发基孔肯雅病毒复制抑制剂

麦考酚酸(MPA)先前已被报道为筑波谷病毒(CHIKV)的抑制剂,其EC 50值为0.2μM。在典型的药物化学程序中,我们使用MPA作为先导化合物来设计和合成一系列的isatins和benzolactones。19种衍生物的合成和测试产生的化合物没有所需的活性,这促使我们重新测试了主要化合物MPA。我们可以揭示MPA没有显示抗Chikv活性,因此需要重新评估它作为该靶标的先导化合物。

更新日期:2017-12-28
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