Enlarging the chemical space of anti-leishmanials: a structure-activity relationship study of peptoids against Leishmania mexicana, a causative agent of cutaneous leishmaniasis

Bolt, H.L.; Eggimann, G.A.; Denny, P.W.; Cobb, S.L.

doi:10.1039/c6md00060f

Enlarging the chemical space of anti-leishmanials: a structure-activity relationship study of peptoids against Leishmania mexicana, a causative agent of cutaneous leishmaniasis

Bolt, H.L.; Eggimann, G.A.; Denny, P.W.; Cobb, S.L.

Authors

H.L. Bolt

G.A. Eggimann

Professor Paul Denny p.w.denny@durham.ac.uk
Professor

Professor Steven Cobb s.l.cobb@durham.ac.uk
Professor

Abstract

Peptoids, a class of peptide mimetics, have emerged as promising anti-infective agents against a range of bacterial and fungal infections. Recently we have shown peptoids to be novel anti-parasitic and, specifically, anti-leishmanial, compounds. In this study, we have expanded the chemical space of our peptoid library and have identified peptoids with low micromolar activity against Leishmania mexicana axenic amastigotes and significantly, the first peptoids with promising activity against intracellular amastigotes, which are the clinical cause of cutaneous leishmaniasis.

Citation

Bolt, H., Eggimann, G., Denny, P., & Cobb, S. (2016). Enlarging the chemical space of anti-leishmanials: a structure-activity relationship study of peptoids against Leishmania mexicana, a causative agent of cutaneous leishmaniasis. MedChemComm, 7(5), 799-805. https://doi.org/10.1039/c6md00060f

Journal Article Type	Article
Acceptance Date	Mar 10, 2016
Online Publication Date	Mar 15, 2016
Publication Date	May 1, 2016
Deposit Date	Jan 27, 2016
Publicly Available Date	Mar 31, 2016
Journal	MedChemComm.
Print ISSN	2040-2503
Electronic ISSN	2040-2511
Publisher	Royal Society of Chemistry
Peer Reviewed	Peer Reviewed
Volume	7
Issue	5
Pages	799-805
DOI	https://doi.org/10.1039/c6md00060f