1,3,5-Triazino Peptide Derivatives: Synthesis, Characterization, and Preliminary Antileishmanial Activity.
Sherine N KhattabHosam H KhalilAdnan A BekhitMohamed M Abd El-RahmanBeatriz G de la TorreMatti HaukkaFernando AlbericioPublished in: ChemMedChem (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.
Keyphrases
- mass spectrometry
- ms ms
- liquid chromatography
- high resolution
- high performance liquid chromatography
- structure activity relationship
- gas chromatography
- capillary electrophoresis
- solid phase extraction
- liver failure
- oxidative stress
- drug induced
- simultaneous determination
- pseudomonas aeruginosa
- respiratory failure
- ionic liquid
- acute respiratory distress syndrome
- molecular dynamics simulations
- extracorporeal membrane oxygenation
- mechanical ventilation