pyrimidinones and Trypanosomiasis--African

pyrimidinones has been researched along with Trypanosomiasis--African* in 1 studies

Other Studies

1 other study(ies) available for pyrimidinones and Trypanosomiasis--African

Article	Year
Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity. Journal of medicinal chemistry, 2015, Oct-22, Volume: 58, Issue:20 The bifunctional enzyme N(5),N(10)-methylenetetrahydrofolate dehydrogenase/cyclo hydrolase (FolD) is essential for growth in Trypanosomatidae. We sought to develop inhibitors of Trypanosoma brucei FolD (TbFolD) as potential antiparasitic agents. Compound 2 was synthesized, and the molecular structure was unequivocally assigned through X-ray crystallography of the intermediate compound 3. Compound 2 showed an IC50 of 2.2 μM, against TbFolD and displayed antiparasitic activity against T. brucei (IC50 49 μM). Using compound 2, we were able to obtain the first X-ray structure of TbFolD in the presence of NADP(+) and the inhibitor, which then guided the rational design of a new series of potent TbFolD inhibitors. Topics: Animals; Crystallography, X-Ray; Drug Design; Enzyme Inhibitors; Humans; Leukemia; Macrophages; Methylenetetrahydrofolate Dehydrogenase (NADP); Models, Molecular; Phenylurea Compounds; Pyrimidinones; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosomiasis, African	2015

Article

Year

Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity.

Journal of medicinal chemistry, 2015, Oct-22, Volume: 58, Issue:20

The bifunctional enzyme N(5),N(10)-methylenetetrahydrofolate dehydrogenase/cyclo hydrolase (FolD) is essential for growth in Trypanosomatidae. We sought to develop inhibitors of Trypanosoma brucei FolD (TbFolD) as potential antiparasitic agents. Compound 2 was synthesized, and the molecular structure was unequivocally assigned through X-ray crystallography of the intermediate compound 3. Compound 2 showed an IC50 of 2.2 μM, against TbFolD and displayed antiparasitic activity against T. brucei (IC50 49 μM). Using compound 2, we were able to obtain the first X-ray structure of TbFolD in the presence of NADP(+) and the inhibitor, which then guided the rational design of a new series of potent TbFolD inhibitors.

Topics: Animals; Crystallography, X-Ray; Drug Design; Enzyme Inhibitors; Humans; Leukemia; Macrophages; Methylenetetrahydrofolate Dehydrogenase (NADP); Models, Molecular; Phenylurea Compounds; Pyrimidinones; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosomiasis, African

2015