Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase,RSC Medicinal Chemistry

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Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2019/12/16 , DOI: 10.1039/c9md00511k
Shams Ul Mahmood _{1,

2,

3,

4} , Huimin Cheng _{1,

2,

3,

4} , Sreedhar R. Tummalapalli _{1,

2,

3,

4} , Ramappa Chakrasali _{1,

2,

3,

4} , Rammohan R. Yadav Bheemanaboina _{1,

2,

3,

4} , Tamara Kreiss _{1,

2,

3,

4} , Agnieska Chojnowski _{1,

2,

3,

4} , Tyler Eck _{1,

2,

3,

4} , John J. Siekierka _{1,

2,

3,

4} , David P. Rotella _{1,

2,

3,

4}

Affiliation

The cGMP-dependent protein kinase in Plasmodium falciparum (PfPKG) plays multiple roles in the life cycle of the parasite. As a result, this enzyme is a potential target for new antimalarial agents. Existing inhbitors, while potent and active in malaria models are not optimal. This communication describes initial optimization of a structurally distinct class of PfPKG inhibitors.

中文翻译：

发现基于恶唑基的恶性疟原虫cGMP依赖性蛋白激酶抑制剂

恶性疟原虫（PfPKG）中依赖于cGMP的蛋白激酶在寄生虫的生命周期中起着多种作用。结果，该酶是新抗疟药的潜在靶标。现有的抑制因素虽然在疟疾模型中有效且活跃，但并不是最佳的。该通报描述了结构上不同的PfPKG抑制剂类别的初始优化。

更新日期：2020-02-13

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