Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase

Autor:	Alex Musso Buendía, Alessandro Schipani, Dolores Gonzalez Pacanowska, Orla K. Mc Carthy, Luis M. Ruiz-Pérez, Reto Brun, Marcel Kaiser, Ian H. Gilbert
Rok vydání:	2006
Předmět:	Stereochemistry Trypanosoma cruzi Clinical Biochemistry Pharmaceutical Science Biochemistry Inhibitory Concentration 50 chemistry.chemical_compound DUTP pyrophosphatase Acetamides parasitic diseases Drug Discovery Peptide synthesis Animals Chagas Disease Amino Acids Enzyme Inhibitors Pyrophosphatases Uracil Molecular Biology chemistry.chemical_classification Dipeptide biology Organic Chemistry biology.organism_classification Trypanocidal Agents Amino acid Models Chemical chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Acetamide
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:3809-3812
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2006.04.027
Popis:	Potential inhibitors of the Trypanosoma cruzi dUTP nucleotidohydrolase were docked into the enzyme using the program FlexX. Compounds that docked selectively were then selected and synthesized using solid phase methodology, giving rise to a novel library of amino acid uracil acetamide compounds which were evaluated for enzyme inhibition and anti-parasitic activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::876734f3e2d26e47a398aed67fdca0d6 https://doi.org/10.1016/j.bmcl.2006.04.027 Zobrazit plný text záznamu Full Text from ScienceDirect