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1,3,5-Triazino Peptide Derivatives: Synthesis, Characterization, and Preliminary Antileishmanial Activity

Abstract:

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.