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Pharmaceuticals
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Advances in Antiparasitic Drug Research
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Advances in Antiparasitic Drug Research

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 31 August 2025 | Viewed by 1140

Special Issue Editors

Dr. Andre Aires

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Guest Editor
Department of Tropical Medicine, Health Sciences Center, Federal University of Pernambuco (UFPE), Avenida Prof. Moraes Rego, s/n, Cidade Universitária, Recife 50740-600, PE, Brazil
Interests: schistosomiasis
Prof. Dr. Maria Cristiano

E-Mail Website
Guest Editor
1. Centre of Marine Sciences (CCMAR), University of Algarve, Campus de Gambelas, 8005-139 Faro, Portugal
2. Department of Chemistry and Pharmacy, Faculty of Science and Technology, University of Algarve, Campus de Gambelas, 8005-139 Faro, Portugal
Interests: physical organic chemistry; organic reactivity; medicinal chemistry; bioactive heterocyclic compounds; antiparasitic compounds

Special Issue Information

Dear Colleagues,

The field of antiparasitic drug research has witnessed substantial advancements in recent times. People have successfully developed new compounds with higher specificity and efficacy, significantly reducing side effects and enhancing patient compliance. Breakthroughs in our understanding of parasite genetics and biology have facilitated the identification of novel drug targets, leading to the creation of drugs that effectively combat resistant strains.

Despite these achievements, challenges persist. The complex life cycles of many parasites and their ability to evade host immune responses pose significant hurdles. Additionally, the limited resources and infrastructure in endemic regions pose barriers to the effective distribution and use of these drugs. Continued research is crucial to address these challenges, ensuring that antiparasitic drugs remain effective and accessible in the fight against parasitic diseases.

We invite scholars to contribute their groundbreaking research to this vibrant field, with the aim of fostering collaborative efforts to overcome existing challenges and propel antiparasitic drug research to unprecedented heights.

Dr. Andre Aires
Prof. Dr. Maria Cristiano
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • antiparasitic drug
  • novel drug targets
  • parasite resistance
  • drug efficacy
  • parasite genetics

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Related Special Issue

Published Papers (2 papers)

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Research

14 pages, 2040 KiB  
Article
Phenotypic Screening of H1-Antihistamines Identifies Promethazine and Rupatadine as Active Compounds Against Toxocara canis Infective Larvae
by Taís C. Silva, Julia Godoy-Silva, Monique C. Amaro, João V. Silva-Silva, Thiago H. Doring, Leonardo L. G. Ferreira, Adriano D. Andricopulo and Josué de Moraes
Pharmaceuticals 2025, 18(7), 997; https://doi.org/10.3390/ph18070997 - 2 Jul 2025
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Abstract
Background: Parasitic worm infections remain among the most prevalent and neglected health issues worldwide, affecting both humans and animals. Toxocariasis, caused by Toxocara spp., is a widespread zoonosis with significant public health and economic implications. Current anthelmintic treatments show limited efficacy, particularly [...] Read more.
Background: Parasitic worm infections remain among the most prevalent and neglected health issues worldwide, affecting both humans and animals. Toxocariasis, caused by Toxocara spp., is a widespread zoonosis with significant public health and economic implications. Current anthelmintic treatments show limited efficacy, particularly against tissue-migrating larvae, underscoring the urgent need for new therapeutic options. This study aimed to evaluate the anthelmintic potential of H1 antihistamines as repurposed drug candidates against Toxocara canis. Methods: Twenty-two H1 antihistamines were screened for larvicidal activity against infective third-stage (L3) larvae of T. canis. Larval motility and morphology were assessed, and compounds with the highest efficacy were further investigated using density functional theory (DFT) to explore their electronic properties. Molecular docking simulations were also performed to predict interactions with T. canis β-tubulin. Results: Promethazine and rupatadine exhibited significant larvicidal effects, surpassing albendazole in reducing larval motility and inducing a distinct contorted morphology not observed in control or albendazole-treated larvae. DFT analyses suggested a strong electron-acceptor capacity, indicating a potential redox-based mechanism of action. Docking studies revealed favorable binding to the colchicine site of T. canis β-tubulin. Conclusions: This is the first report of larvicidal activity of antihistamines against T. canis, supporting their potential as repurposed therapeutic agents for the treatment of zoonotic helminthiases, particularly those caused by tissue-migrating nematodes. Full article
(This article belongs to the Special Issue Advances in Antiparasitic Drug Research)
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12 pages, 1788 KiB  
Article
Synthesis and Combination Studies of Novel Dipeptide Nitriles with Curcumin for a Potent Synergistic Action Against Rhodesain, Cysteine Protease of Trypanosoma brucei rhodesiense
by Carla Di Chio, Josè Starvaggi, Santo Previti, Fabiola De Luca, Benito Natale, Sandro Cosconati, Tanja Schirmeister, Maria Zappalà and Roberta Ettari
Pharmaceuticals 2025, 18(6), 847; https://doi.org/10.3390/ph18060847 - 5 Jun 2025
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Abstract
Background/Objectives: Rhodesain is a cysteine protease crucial for the life cycle of Trypanosoma brucei rhodesiense, a parasite that causes the lethal form of human African trypanosomiasis. For these reasons, rhodesain is considered an important target for the drug discovery process of novel [...] Read more.
Background/Objectives: Rhodesain is a cysteine protease crucial for the life cycle of Trypanosoma brucei rhodesiense, a parasite that causes the lethal form of human African trypanosomiasis. For these reasons, rhodesain is considered an important target for the drug discovery process of novel antitrypanosomal agents. Methods: In the present work, we carried out a combination study of two novel synthetic nitriles, Nitrile 1 and Nitrile 2, with curcumin, the golden multitarget nutraceutical obtained from Curcuma longa L., which we demonstrated to inhibit rhodesain in a non-competitive manner. We calculated the combination index (CI) in both the combination studies by using the Chou and Talalay method. Results: Comparing the CI values of the combinations Nitrile 1 + curcumin and Nitrile 2 + curcumin, we assessed that the inhibitory effect of the combination Nitrile 2 + curcumin against rhodesain was much more potent than that of the other combination. At the IC50 value, in the case of the combination Nitrile 1 + curcumin an additive effect occurred, while in the case of Nitrile 2 + curcumin, we observed a moderate synergism: at 99% of the effect, the synergism induced by the combination Nitrile 2 + curcumin was much stronger than the synergism promoted by the combination Nitrile 1 + curcumin (CI = 0.3843 vs 0.6622, respectively). Conclusions: The co-administration of dipeptide nitriles with curcumin enhances rhodesain inhibition through synergistic effects. Notably, Nitrile 2 + curcumin exhibits a stronger synergy at higher inhibition levels, indicating a greater therapeutic potential. Full article
(This article belongs to the Special Issue Advances in Antiparasitic Drug Research)
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