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ChemMedChem ; 13(7): 725-735, 2018 04 06.
Article in English | MEDLINE | ID: mdl-29388337

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.


Subject(s)
Antiprotozoal Agents/pharmacology , Leishmania/drug effects , Peptides/pharmacology , Triazines/pharmacology , Animals , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/toxicity , Chlorocebus aethiops , Male , Mice , Molecular Structure , Peptides/chemical synthesis , Peptides/chemistry , Peptides/toxicity , Structure-Activity Relationship , Triazines/chemical synthesis , Triazines/chemistry , Triazines/toxicity , Vero Cells
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