Jump to main content
Jump to site search

Issue 9, 2014
Previous Article Next Article

Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents

Author affiliations

Abstract

Cyclohexapeptide analogs of natural products were obtained in very good yields by a combination of solid-phase peptide synthesis, for the linear peptide, and solution cyclization. The activities against Plasmodium falciparum K1, Trypanosoma brucei brucei and murine macrophages (cell line J774) of these novel compounds and azolic macrocycles, previously reported by us, were evaluated. Seven macrocycles showed submicromolar activities against Plasmodium falciparum K1 and a high selectivity (SI > 125) for the parasite. In addition, two compounds displayed one digit micromolar EC50 against T. brucei brucei and satisfactory selectivity (SI 82 and 95). Preliminary structure–activity relationships are presented.

Graphical abstract: Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents

Back to tab navigation

Supplementary files

Publication details

The article was received on 24 Mar 2014, accepted on 15 May 2014 and first published on 16 May 2014


Article type: Concise Article
DOI: 10.1039/C4MD00135D
Author version
available:
Download author version (PDF)
Citation: Med. Chem. Commun., 2014,5, 1309-1316

  •   Request permissions

    Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents

    S. Peña, C. Fagundez, A. Medeiros, M. Comini, L. Scarone, D. Sellanes, E. Manta, J. Tulla-Puche, F. Albericio, L. Stewart, V. Yardley and G. Serra, Med. Chem. Commun., 2014, 5, 1309
    DOI: 10.1039/C4MD00135D

Search articles by author

Spotlight

Advertisements