Solid Phase Synthesis and Antiparasitic Activity of a Library of Peptidyl Metronidazoles

A number of peptidyl metronidazole derivatives were synthesized in 99% yield through solid phase peptide synthesis. the newly prepared compounds were tested against entamoeba histolytica and giardia intestinalis and were found to be much less active than metronidazole against the aforementioned parasites; apparently the introduction of the peptide moiety on the metronidazole nucleus has an adverse effect on their antiparasitic activities. nevertheless, grafting metronidazole with amino acids opens the window for parallel screening and combinatorial approaches.