Title: 1,3,5-Triazino Peptide Derivatives: Synthesis, Characterization, and Preliminary Antileishmanial Activity
Authors: Khattab SN, Khalil HH, Bekhit AA, Abd El-Rahman MM, de la Torre BG, El-Faham A, Albericio F.
Journal: ChemMedChem.,doi: 10.1002/cmdc.201700770: (2018)
A library of short di-, tri-, and tetra-peptides with an s-triazine moiety at the N?terminus and either an amide or ethyl ester C?terminus was prepared in solution and on the solid phase. The two remaining positions of the s-triazine moiety were substituted with methoxy, morpholino, or piperidino groups.
All the synthesized peptide derivatives were analyzed by HPLC and fully characterized by IR spectroscopy, 1 H and 13 C?NMR spectroscopy, elemental analysis, and mass spectrometry (MALDI TOF/TOF).
A preliminary study of the antileishmanial activity of the 1,3,5-triazinyl peptide derivatives revealed that four dipeptide amide derivatives showed higher antipromastigote or antiamastigote activity than the reference standard drug miltefosine with no significance acute toxicity.