Design, Synthesis, In Vitro and In Silico Biological Evaluation of New Pyridine-2,5-Dicarboxylates Esters Bearing Natural Source Fragments as Anti-Trypanosomatid Agents.

ABSTRACT: Background: Chagas disease and leishmaniasis remain public health concerns. Despite the existence of approved medications for the treatment of these diseases, most patients discontinue treatment due to long drug regimens and/or the severe side effects of these drugs. This leads to treatment failure and potential future drug resistance. Therefore, the search for new molecules with trypanocidal activity, low cytotoxicity, and high selectivity is essential to address this challenge. Methods: In this work, three series (a, b, and c) of pyridine-2,5-dicarboxylate esters were synthesized using different β-keto-esters bearing naturally occurring fragments and 1,2,3-triazine-1-oxides via the inverse electron demand Diels-Alder (IEDDA) reaction. The structural elucidation of the compo

SUBMITTER: Sanchez-Palestino LM 

PROVIDER: S-EPMC12566703 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature