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

European Journal of Medicinal Chemistry

Volumn 126, Issue , 2017, Pages 72-83

  Azeredo, Luís Felipe S P ^a,b   Coutinho, Julia P ^a,c   Jabor, Valquiria A P ^d   Feliciano, Patricia R ^d   Nonato, Maria Cristina ^d   Kaiser, Carlos R ^b   Menezes, Carla Maria S ^a   Hammes, Amanda S O ^a   Caffarena, Ernesto Raul ^a   Hoelz, Lucas V B ^a   de Souza, Nicolli B ^a   Pereira, Glaécia A N ^a   Cerávolo, Isabela P ^a   Krettli, Antoniana U ^a,c   Boechat, Nubia ^a,b  

^a INSTITUTO OSWALDO CRUZ   (Brazil)

^b FEDERAL UNIVERSITY OF RIO DE JANEIRO   (Brazil)

^c FEDERAL UNIVERSITY OF MINAS GERAIS   (Brazil)

^d UNIVERSITY OF SÃO PAULO   (Brazil)

Author keywords

Dihydroorotate dehydrogenase (DHODH); Malaria; Molecular docking; P. falciparum; Pyrazolo 1,5 a pyrimidine

Indexed keywords

2 METHYL 5 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDIN 7(4H) ONE; 2 METHYL 7 (NAPHTHALEN 2 YLAMINE) 5 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; 2 METHYL 7 PHENYLAMINE 5 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; 2,5 DIMETHYL 7 (NAPHTHALEN 2 YLAMINE)PYRAZOLO [1,5 A]PYRIMIDINE; 2,5 DIMETHYL 7 [2 (TRIFLUOROMETHYL)PHENYLAMINE] PYRAZOLO [1,5 A]PYRIMIDINE; 2,5 DIMETHYL 7 [4 (TRIFLUOROMETHYL)PHENYLAMINE] PYRAZOLO [1,5 A]PYRIMIDINE; 2,5 DIMETHYLPYRAZOLO [1,5 A]PYRIMIDIN 7(4H) ONE; 5 METHYL 2 (TRIFLUOROMETHYL) 7 [2 (TRIFLUOROMETHYL)PHENYLAMINE]PYRAZOLO [1,5 A]PYRIMIDINE; 5 METHYL 2 (TRIFLUOROMETHYL) 7 [4 (TRIFLUOROMETHYL)PHENYLAMINE]PYRAZOLO [1,5 A]PYRIMIDINE; 5 METHYL 2 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDIN 7(4H) ONE; 5 METHYL 7 (NAPHTHALEN 2 YLAMINE) 2 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDIN; 5 METHYL 7 PHENYLAMINE 2 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; 7 (3,5 DIMETHOXYPHENYLAMINE) 2 METHYL 5 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; 7 (3,5 DIMETHOXYPHENYLAMINE) 2,5 DIMETHYLPYRAZOLO [15 A]PYRIMIDINE; 7 (3,5 DIMETHOXYPHENYLAMINE) 5 METHYL 2 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; 7 (4 CHLOROPHENYLAMINE) 2,5 DIMETHYLPYRAZOLO [1,5 A]PYRIMIDINE; 7 (4 CHLOROPHENYLAMINE) 5 METHYL 2 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; 7 CHLORO 2,5 DIMETHYLPYRAZOLO [1,5 A]PYRIMIDINE; 7 CHLORO 5 METHYL 2 (TRIFLUOROMETHYL)PYRAZOLO [1,5 A]PYRIMIDINE; ANTIMALARIAL AGENT; DIHYDROOROTATE DEHYDROGENASE INHIBITOR; UNCLASSIFIED DRUG; DIHYDROOROTATE DEHYDROGENASE; ENZYME INHIBITOR; OXIDOREDUCTASE; PYRIMIDINE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL ACTIVITY; ARTICLE; CARBON NUCLEAR MAGNETIC RESONANCE; CONTINUOUS CULTURE; CONTROLLED STUDY; DRUG SCREENING; ENZYME INHIBITION; HUMAN; IC50; IN VITRO STUDY; MOLECULAR DOCKING; MOLECULAR HYBRIDIZATION; MOUSE; NONHUMAN; PLASMODIUM BERGHEI INFECTION; PLASMODIUM FALCIPARUM; PROTON NUCLEAR MAGNETIC RESONANCE; STATIC ELECTRICITY; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL LINE; CHEMISTRY; DRUG EFFECTS; ENZYMOLOGY; METABOLISM; PRECLINICAL STUDY; PROTEIN CONFORMATION;

ANIMALS; ANTIMALARIALS; CELL LINE; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; MICE; MOLECULAR DOCKING SIMULATION; OXIDOREDUCTASES ACTING ON CH-CH GROUP DONORS; PLASMODIUM FALCIPARUM; PROTEIN CONFORMATION; PYRIMIDINES;

EID: 84991780762     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2016.09.073     Document Type: Article

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