ArticleAntimicrobial agents and chemotherapy2016
Antimalarial Activity of Small-Molecule Benzothiazole Hydrazones.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- The acute oral toxicity and pharmacokinetic determination of a novel chloroquinoline hybrid molecule by LC-MS/MS.Bioanalysis · 2025Article
- Hydrazones, hydrazones-based coinage metal complexes, and their biological applications.RSC advances · 2025Review
- Article
- A Review on Synthetic Thiazole Derivatives as an Antimalarial Agent.Current drug discovery technologies · 2024Review
- Synthesis, characterization, DFT, antioxidant, antibacterial, pharmacokinetics and inhibition of SARS-CoV-2 main protease of some heterocyclic hydrazones.Journal of molecular structure · 2022Article
- Article
- Modern Approaches to the Synthesis and Transformations of Practically Valuable Benzothiazole Derivatives.Molecules (Basel, Switzerland) · 2021Review
- Synthesis of biologically active derivatives of 2-aminobenzothiazole.Chemistry of heterocyclic compounds · 2021Article
- An epigrammatic status of the 'RSC medicinal chemistry · 2020Review
- Article
- The Trypanosomal Transferrin Receptor of Trypanosoma Brucei-A Review.Tropical medicine and infectious disease · 2019Review
- Slight changes in the chemical structure of haemanthamine greatly influence the effect of the derivatives on rumen fermentation in vitro.Scientific reports · 2019Article
- Synthesis and Antidepressant Activity Profile of Some Novel Benzothiazole Derivatives.Molecules (Basel, Switzerland) · 2017Article
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10 authors.
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No grant is acknowledged in the PubMed record.
Abstract
We synthesized a new series of conjugated hydrazones that were found to be active against malaria parasite in vitro, as well as in vivo in a murine model. These hydrazones concentration-dependently chelated free iron and offered antimalarial activity. Upon screening of the synthesized hydrazones, compound 5f was found to be the most active iron chelator, as well as antiplasmodial. Compound 5f also interacted with free heme (KD [equilibrium dissociation constant] = 1.17 ± 0.8 μM), an iron-containing tetrapyrrole released after hemoglobin digestion by the parasite, and inhibited heme polymerization by parasite lysate. Structure-activity relationship studies indicated that a nitrogen- and sulfur-substituted five-membered aromatic ring present within the benzothiazole hydrazones might be responsible for their antimalarial activity. The dose-dependent antimalarial and heme polymerization inhibitory activities of the lead compound 5f were further validated by following [(3)H]hypoxanthine incorporation and hemozoin formation in parasite, respectively. It is worth mentioning that compound 5f exhibited antiplasmodial activity in vitro against a chloroquine/pyrimethamine-resistant strain of Plasmodium falciparum (K1). We also evaluated in vivo antimalarial activity of compound 5f in a murine model where a lethal multiple-drug-resistant strain of Plasmodium yoelii was used to infect Swiss albino mice. Compound 5f significantly suppressed the growth of parasite, and the infected mice experienced longer life spans upon treatment with this compound. During in vitro and in vivo toxicity assays, compound 5f showed minimal alteration in biochemical and hematological parameters compared to control. In conclusion, we identified a new class of hydrazone with therapeutic potential against malaria.
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