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Antiprotozoal Agents01:21

Antiprotozoal Agents

Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...
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Antiviral Nucleoside Inhibitors01:22

Antiviral Nucleoside Inhibitors

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Updated: May 28, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
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Published on: August 6, 2020

Hydroxamic Acids as HDAC Inhibitor Drug Leads for Malaria.

Wisam A Dawood1,2, Jacinta R Macdonald1,2, Christian Anzenhofer3

  • 1Institute for Biomedicine and Glycomics, Griffith University, Southport, Queensland, Australia.

Medicinal Research Reviews
|May 26, 2026
PubMed
Summary
This summary is machine-generated.

Histone deacetylase inhibitors show promise for combating malaria, a significant global health issue. Research reviews over 750 compounds, offering insights into developing new antimalarial drugs against Plasmodium falciparum.

Keywords:
HDAC inhibitorPlasmodiumhydroxamic acidmalariastructure‐activity relationship

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Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
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Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
09:20

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS

Published on: August 10, 2017

Area of Science:

  • Parasitology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Malaria remains a critical global health challenge, causing millions of cases and deaths annually, primarily in Sub-Saharan Africa.
  • Plasmodium falciparum is the deadliest malaria parasite, and drug resistance significantly impedes eradication efforts.
  • Novel therapeutic strategies are essential to overcome drug resistance and develop effective malaria treatments.

Purpose of the Study:

  • To review the potential of histone deacetylase (HDAC) inhibitors as antimalarial drug leads.
  • To assess the antiplasmodial activity and structure-activity relationships of hydroxamic acid derivatives against P. falciparum.
  • To guide future drug discovery efforts by analyzing potency, selectivity, and physicochemical properties of HDAC inhibitors.

Main Methods:

  • Comprehensive literature review of HDAC inhibitors with published in vitro activity against P. falciparum.
  • Analysis of structure-activity relationships for over 750 hydroxamic acid compounds.
  • Evaluation of compound potency, selectivity, and physicochemical characteristics.

Main Results:

  • HDACs are identified as promising drug targets due to their essential roles in Plasmodium parasite regulation.
  • Extensive structure-activity relationship data for hydroxamic acids provide insights into antimalarial efficacy.
  • Comparative analysis reveals key properties influencing the potential of this chemotype as antimalarial drug leads.

Conclusions:

  • HDAC inhibitors represent a viable class of compounds for developing new antimalarial therapies.
  • The reviewed data offer a foundation for optimizing existing compounds and designing novel HDAC inhibitors.
  • Further investigation into this chemotype could lead to effective treatments for malaria and other parasitic diseases.