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)
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.
This file is not available for download.
Citation: Khattab SN, Khalil HH, Bekhit AA, Abd El-Rahman MM, de la Torre BG, El-Faham A, Albericio F. 1,3,5-Triazino Peptide Derivatives: Synthesis, Characterization, and Preliminary Antileishmanial Activity ChemMedChem.,doi: 10.1002/cmdc.201700770: (2018).