1,3,5‐Triazino Peptide Derivatives: Synthesis,Characterization, and Preliminary Antileishmanial Activity |
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| Authors: | Prof Sherine N Khattab Dr Hosam H Khalil Prof Adnan A Bekhit Prof Mohamed M Abd?El‐Rahman Prof Beatriz G de?la?Torre Prof Ayman El‐Faham Prof Fernando Albericio |
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| Affiliation: | 1. Department of Chemistry, Faculty of Science, Alexandria University, Ibrahimia, Alexandria, Egypt;2. Cancer Nanotechnology Research Laboratory(CNRL), Faculty of Pharmacy, Alexandria University, Alexandria, Egypt;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt;4. KRISP, School of Health Sciences, University of KwaZulu-Natal, Durban, South Africa;5. Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia;6. School of Chemistry and Physics, University of KwaZulu-Natal, Durban, South Africa;7. CIBER-BBN, Networking Centre on Bioengineering Biomaterials and Nanomedicine, Barcelona, Spain;8. Department of Organic Chemistry, University of Barcelona, Barcelona, Spain |
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| 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, 1H and 13C 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. |
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| Keywords: | 1 3 5-triazine derivatives antileishmanial compounds morpholines peptides piperidines |
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