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首页> 外文期刊>Archiv der Pharmazie >Diarylpyrazole Ligated Dihydropyrimidine Hybrids as Potent Non-Classical Antifolates and Their Efficacy Against Plasmodium falciparum
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Diarylpyrazole Ligated Dihydropyrimidine Hybrids as Potent Non-Classical Antifolates and Their Efficacy Against Plasmodium falciparum

机译：二芳基吡唑连接的二氢嘧啶杂交物作为有效的非古典防雾及其对疟原虫的疗效

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摘要

A series of diarylpyrazole clubbed dihydropyrimidine derivatives (J1-J30) was synthesized under microwave-assisted heating conditions by employing Biginelli reaction methodology and utilizing triethylammonium acetate both as a catalyst and as reaction medium, leading towards a greener reaction pathway. The synthesized entities were screened for their antimalarial efficacy against a Plasmodium falciparum strain in vitro. The active entities (J9, J15, J21, J25, and J27) obtained out of the in vitro screening were further evaluated for their enzyme inhibitory potency against the Pf-DHFR enzyme in vitro as well as in silico using Glide. Furthermore, the active scaffolds were tested for their cytotoxicity against Vero cells, proving their nontoxic behavior and selectivity. The ADME parameters were also evaluated and predicted in silico, indicating good oral bioavailability of the compounds.
机译：通过使用Biginelli反应方法并利用作为催化剂的三乙基铵和作为反应介质，在微波辅助的加热条件下合成了一系列二芳基吡唑杆菌衍生物（J1-J30）。 筛选合成实体，用于对体外疟原虫菌株的抗疟药效果。 在体外筛选中获得的活性实体（J9，J15，J21，J25和J27）在体外抑制PF-DHFR酶的酶抑制效力以及使用滑翔的硅基溶液。 此外，将活性支架对其对Vero细胞进行细胞毒性的测试，证明它们的无毒行为和选择性。 在硅中还评估并预测了ADME参数，表明化合物的良好口服生物利用度。

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