Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To Inhibit Trypanosoma brucei Pteridine Reductase in Support of Early-Stage Drug Discovery

[Image: see text] Pteridine reductase-1 (PTR1) is a promising drug target for the treatment of trypanosomiasis. We investigated the potential of a previously identified class of thiadiazole inhibitors of Leishmania major PTR1 for activity against Trypanosoma brucei (Tb). We solved crystal structures...

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Veröffentlicht in:ACS Omega
Hauptverfasser: Linciano, Pasquale, Dawson, Alice, Pöhner, Ina, Costa, David M., Sá, Monica S., Cordeiro-da-Silva, Anabela, Luciani, Rosaria, Gul, Sheraz, Witt, Gesa, Ellinger, Bernhard, Kuzikov, Maria, Gribbon, Philip, Reinshagen, Jeanette, Wolf, Markus, Behrens, Birte, Hannaert, Véronique, Michels, Paul A. M., Nerini, Erika, Pozzi, Cecilia, di Pisa, Flavio, Landi, Giacomo, Santarem, Nuno, Ferrari, Stefania, Saxena, Puneet, Lazzari, Sandra, Cannazza, Giuseppe, Freitas-Junior, Lucio H., Moraes, Carolina B., Pascoalino, Bruno S., Alcântara, Laura M., Bertolacini, Claudia P., Fontana, Vanessa, Wittig, Ulrike, Müller, Wolfgang, Wade, Rebecca C., Hunter, William N., Mangani, Stefano, Costantino, Luca, Costi, Maria P.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2017
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5623949/
https://ncbi.nlm.nih.gov/pubmed/28983525
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsomega.7b00473
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