7H-Pyrrolo[2,3-d]pyrimidine-4-amines as Potential Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinases,ChemMedChem

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7H-Pyrrolo[2,3-d]pyrimidine-4-amines as Potential Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinases
ChemMedChem ( IF 3.6 ) Pub Date : 2022-09-15 , DOI: 10.1002/cmdc.202200421
Tswene D Seanego _{1,

2} , Hlamulo E Chavalala _{1,

2} , Hendrik H Henning ₁ , Charles B de Koning ₁ , Heinrich C Hoppe ₃ , Kayode K Ojo ₄ , Amanda L Rousseau _{1,

2}

Affiliation

Hitting malaria where it hurts: Pyrrolo[2,3-d]pyrimidines have been designed as potential inhibitors targeting Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) using molecular modelling. Compounds displaying good binding interactions in silico were synthesised and assessed for inhibitory activity against PfCDPK4 and PfCDPK1, with several compounds displaying promising inhibitory activity against either PfCDPK4 (IC₅₀=0.210–0.530 μM), or PfCDPK1 (IC₅₀=0.589 μM).

中文翻译：

7H-吡咯并[2,3-d]嘧啶-4-胺作为恶性疟原虫钙依赖性蛋白激酶的潜在抑制剂

直击疟疾痛处：吡咯并[2,3- d ]嘧啶已被设计为针对恶性疟原虫钙依赖性蛋白激酶 4 ( Pf CDPK4) 的潜在抑制剂。合成了在计算机模拟中表现出良好结合相互作用的化合物，并评估了其对Pf CDPK4 和Pf CDPK1 的抑制活性，其中几种化合物对Pf CDPK4 (IC ₅₀ =0.210–0.530 μM) 或Pf CDPK1 (IC ₅₀ =0.589)显示出有希望的抑制活性。微米）。

更新日期：2022-09-15

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