Title
Novel Diacyl-hydrazide Compounds as Potential Therapeutics for Visceral Leishmaniasis
Author
Rebecca Zheng
Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University
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Abstract
Visceral leishmaniasis is a neglected tropical disease with the highest mortality among different forms of leishmaniasis manifestation in humans. The disease is caused by the parasitic protists Leishmania donovani and Leishmania infantum, and treatments remain unsuitable due to high costs, complicated administration, lack of efficacy, variable patient susceptibility, toxic side effects, and rising parasitic resistance. Herein, we report a structure–activity relationship (SAR) exploration of the diacyl-hydrazide scaffold identified to have antiparasitic activity from a high-throughput screen against L. donovani, Trypanosoma cruzi, and Trypanosoma brucei. This SAR study revealed new structural insights into this scaffold related to bioactivity resulting in a new series of lead compounds with nanomolar activity against L. donovani and no toxicity against human THP-1 macrophages. These optimized diacyl-hydrazide compounds set the stage for future drug development and hold promise for a new treatment avenue for visceral leishmaniasis.
Keywords
EthanolEthyl groupsHigh-performance liquid chromatographyModificationParasites
Object type
Language
English [eng]
Persistent identifier
Appeared in
Title
ACS Omega
Volume
9
Issue
35
ISSN
2470-1343
Issued
2024
From page
37170
To page
37182
Publication
American Chemical Society (ACS)
Version type
Date issued
2024
Access rights
Rights
Rights statement
© 2024 The Authors
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