Evaluation of 7-arylaminopyrazolo[1,5-a]pyrimidines as anti-Plasmodium falciparum, antimalarial, and Pf-dihydroorotate dehydrogenase inhibitors

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• 作者：Luí ; s Felipe S.P. Azeredo^a ; ^b ; Julia P. Coutinho^c ; ^d ; Valquiria A.P. Jabor^e ; Patricia R. Feliciano^e ; Maria Cristina Nonato^e ; Carlos R. Kaiser^b ; Carla Maria S. Menezes^a ; Amanda S.O. Hammes^f ; Ernesto Raul Caffarena^f ; Lucas V.B. Hoelz^a ; Nicolli B. de Souza^c ; Glaé ; cia A.N. Pereira^c ; Isabela P. Cerá ; volo^c ; Antoniana U. Krettli^c ; ^d ; Nubia Boechat^a ; ^b ; ^{boechat@far.fiocruz.br}
• 关键词：Malaria ; P. falciparum ; Pyrazolo[1 ; 5-a]pyrimidine ; Dihydroorotate dehydrogenase (DHODH) ; Molecular docking
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：72-83
• 全文大小：1374 K
• 卷排序：126

文摘

7-arylpyrazolo[1,5-a]pyrimidines were designed and synthesized as antiplasmodial. Compounds were tested against P. falciparum as antimalarial and as PfDHODH inhibitors. In P. falciparum the IC50 values have been from 1.2 to 88.2 μM. Parasitemia in P. berghei was reduced by 50% on the 5th day inoculation. The docking results agreed with the values obtained from enzymatic assays.