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  • Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae of Haemonchus contortus In Vitro

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    Author(s)
    Herath, HMP Dilrukshi
    Taki, Aya C
    Nghi, Nguyen
    Garcia-Bustos, Jose
    Hofmann, Andreas
    Wang, Tao
    Ma, Guangxu
    Chang, Bill CH
    Jabbar, Abdul
    Sleebs, Brad E
    Gasser, Robin B
    Griffith University Author(s)
    Hofmann, Andreas
    Year published
    2020
    Metadata
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    Abstract
    Parasitic roundworms (nematodes) are significant pathogens of humans and animals and cause substantive socioeconomic losses due to the diseases that they cause. The control of nematodes in livestock animals relies heavily on the use of anthelmintic drugs. However, their extensive use has led to a widespread problem of drug resistance in these worms. Thus, the discovery and development of novel chemical entities for the treatment of parasitic worms of humans and animals is needed. Herein, we describe our medicinal chemistry optimization efforts of a phenotypic hit against Haemonchus contortus based on a pyrrolidine-oxadiazole ...
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    Parasitic roundworms (nematodes) are significant pathogens of humans and animals and cause substantive socioeconomic losses due to the diseases that they cause. The control of nematodes in livestock animals relies heavily on the use of anthelmintic drugs. However, their extensive use has led to a widespread problem of drug resistance in these worms. Thus, the discovery and development of novel chemical entities for the treatment of parasitic worms of humans and animals is needed. Herein, we describe our medicinal chemistry optimization efforts of a phenotypic hit against Haemonchus contortus based on a pyrrolidine-oxadiazole scaffold. This led to the identification of compounds with potent inhibitory activities (IC50 = 0.78–22.4 μM) on the motility and development of parasitic stages of H. contortus, and which were found to be highly selective in a mammalian cell counter-screen. These compounds could be used as suitable chemical tools for drug target identification or as lead compounds for further optimization.
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    Journal Title
    Molecules
    Volume
    25
    Issue
    8
    DOI
    https://doi.org/10.3390/molecules25082004
    Copyright Statement
    © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
    Subject
    Medicinal and biomolecular chemistry
    Organic chemistry
    Theoretical and computational chemistry
    Science & Technology
    Life Sciences & Biomedicine
    Physical Sciences
    Biochemistry & Molecular Biology
    Chemistry, Multidisciplinary
    Publication URI
    http://hdl.handle.net/10072/396270
    Collection
    • Journal articles

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