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American Society for Microbiology, Antimicrobial Agents and Chemotherapy, 3(61), 2017

DOI: 10.1128/aac.01228-16

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Snapshot Profiling of the Antileishmanial Potency of Lead Compounds and Drug Candidates against Intracellular Leishmania donovani Amastigotes, with a Focus on Human-Derived Host Cells

Journal article published in 2017 by Markela Koniordou, Stephen Patterson, Susan Wyllie, Karin Seifert ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

ABSTRACT This study characterized the in vitro potencies of antileishmanial agents against intracellular Leishmania donovani amastigotes in primary human macrophages, obtained with or without CD14-positive monocyte enrichment, phorbol 12-myristate 13-acetate (PMA)-differentiated THP-1 cells, and mouse peritoneal exudate macrophages (PEMs). Host cell-dependent potency was confirmed for pentavalent and trivalent antimony. Fexinidazole was inactive against intracellular amastigotes across the host cell panel. Fexinidazole sulfone, ( R )-PA-824, ( S )-PA-824, and VL-2098 displayed similar potency in all of the host cells tested.