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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Published in:ACS Omega
Main Authors: 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
Language:Inglês
Published: American Chemical Society 2017
Online Access: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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