{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Lopes A"],"funding":["Funda??o para a Ci?ncia e a Tecnologia","Rede Nacional de RMN","Operacional Programme for Competitiveness and Internationalisation"],"pagination":["1427-1433"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9465711"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["13(9)"],"pubmed_abstract":["Sleeping sickness and leishmaniasis are neglected tropical diseases that threaten millions of people. The currently available therapies present several limitations, including high toxicity, lack of efficacy, and emerging drug resistance, prompting a search for novel therapeutic agents. In this work, we designed, synthesized, and <i>in vitro</i> evaluated the activity of new pyrimido[5,4-<i>d</i>]pyrimidines against <i>Trypanosoma brucei</i> and <i>Leishmania infantum</i> (promastigote and amastigote forms). The cytotoxicity of the compounds against the THP1 cell line was also assessed. Most tested compounds presented low micromolar activity against <i>T. brucei</i> with IC<sub>50</sub> values in the range between 0.9 and 13.4 μM, and one compound also showed activity against <i>L. infantum"],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["Pyrimido[5,4-<i>d</i>]pyrimidine-Based Compounds as a Novel Class of Antitrypanosomal and Antileishmanial Agents."],"pmcid":["PMC9465711"],"funding_grant_id":["PINFRA/22161/2016","UIDB/00686/2020","POCI-01-0145-FEDER-031013"],"pubmed_authors":["Lopes A","Cordeiro-da-Silva A","Santarem N","Carvalho MA"],"additional_accession":[]},"is_claimable":false,"name":"Pyrimido[5,4-<i>d</i>]pyrimidine-Based Compounds as a Novel Class of Antitrypanosomal and Antileishmanial Agents.","description":"Sleeping sickness and leishmaniasis are neglected tropical diseases that threaten millions of people. The currently available therapies present several limitations, including high toxicity, lack of efficacy, and emerging drug resistance, prompting a search for novel therapeutic agents. In this work, we designed, synthesized, and <i>in vitro</i> evaluated the activity of new pyrimido[5,4-<i>d</i>]pyrimidines against <i>Trypanosoma brucei</i> and <i>Leishmania infantum</i> (promastigote and amastigote forms). The cytotoxicity of the compounds against the THP1 cell line was also assessed. Most tested compounds presented low micromolar activity against <i>T. brucei</i> with IC<sub>50</sub> values in the range between 0.9 and 13.4 μM, and one compound also showed activity against <i>L. infantum","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Sep","modification":"2025-04-21T15:14:53.633Z","creation":"2025-04-21T15:14:53.633Z"},"accession":"S-EPMC9465711","cross_references":{"pubmed":["36105326"],"doi":["10.1021/acsmedchemlett.2c00170"]}}