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Pharmaceuticals
Special Issues
Pharmacological Treatments for Parasitic Diseases
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Pharmacological Treatments for Parasitic Diseases

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

Deadline for manuscript submissions: 31 October 2026 | Viewed by 2077

Special Issue Editors

Dr. Maria Dichiara

E-Mail Website
Guest Editor
Department of Drug and Health Sciences, University of Catania, Via Valdisavoia, 5, 95123 Catania, Italy
Interests: medicinal chemistry; synthesis; anticancer; analgesia; hybrid compounds; statistical analysis
Special Issues, Collections and Topics in MDPI journals
Dr. Giuliana Costanzo

E-Mail Website
Guest Editor
Department of Drug and Health Sciences, University of Catania, Via Valdisavoia, 5, 95123 Catania, Italy
Interests: medicinal chemistry; synthesis; analgesia; opioid; HDAC

Special Issue Information

Dear Colleagues,

Parasitic diseases remain a major global health issue, particularly in low- and middle-income countries, where access to healthcare and sanitation is often limited. Diseases such as malaria, leishmaniasis, schistosomiasis, and Chagas disease affect millions of people every year and are leading causes of illness and death. Drug therapies are still limited, with challenges such as toxicity, reduced effectiveness, and the emergence of drug-resistant parasites posing significant obstacles. There is a pressing need for safer, more effective, and innovative treatment options. Advances in molecular biology, drug screening, and bioinformatics are enabling researchers to discover and optimize new antiparasitic drugs.

In this Special Issue, we aim to bring together expert research highlighting therapeutic agents and strategies, as well as identifying future directions that will drive discoveries and new treatments for parasitic diseases. Contributions spanning the fields of medicinal chemistry, pharmacology, parasitology, and global health are especially welcome.

Dr. Maria Dichiara
Dr. Giuliana Costanzo
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 250 words) can be sent to the Editorial Office for assessment.

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

  • parasitic diseases
  • antiparasitic agents
  • drug resistance
  • therapeutic strategies
  • drug discovery
  • neglected tropical diseases (NTDs)
  • medicinal chemistry
  • global health

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Related Special Issues

Published Papers (3 papers)

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Research

17 pages, 2254 KB  
Article
Evaluation of Antiplasmodial Activity of Quinoline Derivatives Incorporating Arylnitro and Aminochalcone Moieties
by Nanang R. Ariefta, Richard M. Beteck, Lesetja J. Legoabe and Yoshifumi Nishikawa
Pharmaceuticals 2026, 19(5), 740; https://doi.org/10.3390/ph19050740 - 8 May 2026
Viewed by 465
Abstract
Background/Objectives: The widespread emergence of chloroquine-resistant Plasmodium falciparum continues to drive the search for new quinoline-based antimalarial agents capable of retaining efficacy against resistant parasites. This study aimed to evaluate a series of synthetic quinoline derivatives incorporating arylnitro and aminochalcone moieties for their [...] Read more.
Background/Objectives: The widespread emergence of chloroquine-resistant Plasmodium falciparum continues to drive the search for new quinoline-based antimalarial agents capable of retaining efficacy against resistant parasites. This study aimed to evaluate a series of synthetic quinoline derivatives incorporating arylnitro and aminochalcone moieties for their antiplasmodial activity and selectivity. Methods: A series of eighteen synthetic quinoline derivatives were evaluated for in vitro antiplasmodial activity against P. falciparum strains (3D7, K1, and Dd2), along with cytotoxicity in mammalian cells and hemolytic activity in human red blood cells. Structure–activity relationship analysis was performed, and molecular docking studies were conducted against β-hematin and the chloroquine resistance transporter (PfCRT). Results: Several compounds exhibited sub-micromolar activity against the chloroquine-sensitive 3D7 strain. The most potent compound (Compound 14), a nitro-substituted N-alkylated quinoline bearing a CF3-enriched aromatic chalcone framework, demonstrated high potency and selectivity (IC50 = 0.13 μM; SI = 1132.92). Importantly, this compound retained substantial activity against multidrug-resistant K1 and Dd2 strains, displaying lower resistance indices than chloroquine. Structure–activity relationship analysis revealed that nitro substitution, N-alkylation, and halogen/CF3-rich aromatic features critically influence potency and selectivity. Docking studies suggested that Compound 14 engages both β-hematin and PfCRT more extensively than chloroquine. Conclusions: These findings identify Compound 14 as a promising lead scaffold for further optimization toward next-generation antimalarial agents. Full article
(This article belongs to the Special Issue Pharmacological Treatments for Parasitic Diseases)
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13 pages, 1841 KB  
Article
Development of a Luciferase-Based In Vitro Assay to Evaluate the Efficacy of Anti-Cryptosporidial Drugs Against Cryptosporidium parvum
by Rie Kubota, Coh-ichi Nihei and Yoshifumi Nishikawa
Pharmaceuticals 2026, 19(4), 576; https://doi.org/10.3390/ph19040576 - 3 Apr 2026
Viewed by 453
Abstract
Background/Objectives: Cryptosporidium parvum is a major causative agent of cryptosporidiosis; however, progress in anti-cryptosporidial drug discovery has been hindered by the lack of robust and reproducible in vitro evaluation systems. In this study, we developed and optimized a luciferase-based in vitro assay [...] Read more.
Background/Objectives: Cryptosporidium parvum is a major causative agent of cryptosporidiosis; however, progress in anti-cryptosporidial drug discovery has been hindered by the lack of robust and reproducible in vitro evaluation systems. In this study, we developed and optimized a luciferase-based in vitro assay to quantitatively monitor C. parvum growth in HCT-8 cells. Methods: Key experimental parameters affecting infection efficiency were systematically examined, including sodium taurocholate treatment, timing of medium replacement, and serum concentration. Results: Sodium taurocholate significantly enhanced parasite infectivity, and removal of non-invaded parasites at 3 h post-infection (hpi) resulted in approximately 2-fold and 3.7-fold increase in luciferase activity at 24 and 48 hpi, respectively, compared with untreated controls. In contrast, removal at 24 hpi led to only an approximately 2.5-fold increase at 48 hpi, consistent with stage-dependent differences in parasite development. Morphological analyses confirmed parasite differentiation from trophozoites to meronts, followed by progression toward sexual stages. Using the optimized assay system, we evaluated several anticoccidial compounds and demonstrated potent in vitro activity of monensin and its structural analog kijimicin, whereas diclazuril and toltrazuril exhibited limited efficacy. Conclusions: Collectively, this luciferase-based platform provides a reliable and quantitative tool for anti-cryptosporidial drug screening and will facilitate future therapeutic development against C. parvum. Full article
(This article belongs to the Special Issue Pharmacological Treatments for Parasitic Diseases)
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24 pages, 10139 KB  
Article
7-Prenyloxycoumarins as Promising Antileishmanial Agents: In Vitro, In Vivo, and In Silico Evaluation Against Leishmania amazonensis
by Dirlei Nico, Daniel Clemente de Moraes, Anna Claudia Silva, Igor Nunes Taveira, Yasmin da Silva Fontes, Rosangela Sabbatini Capella Lopes, Cláudio Cerqueira Lopes and Antonio Ferreira-Pereira
Pharmaceuticals 2026, 19(3), 426; https://doi.org/10.3390/ph19030426 - 5 Mar 2026
Viewed by 705
Abstract
Background/Objectives: Leishmaniasis remains a major neglected tropical disease, and current chemotherapeutic options are limited by toxicity and resistance in Leishmania species, including L. amazonensis. Prenylated coumarins have emerged as promising bioactive scaffolds. Altissimacoumarin D and its analogues inhibit fungal efflux pumps associated [...] Read more.
Background/Objectives: Leishmaniasis remains a major neglected tropical disease, and current chemotherapeutic options are limited by toxicity and resistance in Leishmania species, including L. amazonensis. Prenylated coumarins have emerged as promising bioactive scaffolds. Altissimacoumarin D and its analogues inhibit fungal efflux pumps associated with resistance. However, their antileishmanial potential and mechanisms of action remain unclear. Here, we evaluated the in vitro, in vivo, and in silico effects of altissimacoumarin D and seven analogues against L. amazonensis. Methods: In vitro assays were performed to identify active compounds and assess toxicity in keratinocytes. In vivo experiments in hamsters evaluated antileishmanial activity and renal and hepatic toxicity. In silico analyses were conducted to investigate the mechanism of action of the substances. Results: In vitro assays showed that ACS47, ACS48, and ACS51 were the most active and safe compounds. In a hamster infection model, daily administration of ACS47 and ACS48 (2.5 mg/kg) significantly reduced parasite burden and lesion size, while maintaining normal renal and hepatic biochemical parameters. Histological analysis correlated reduced lesion size with marked decreases in amastigote density. Based on in silico analysis, spermidine synthase was supported as a plausible molecular target. Conclusions: Collectively, these findings identify ACS47 and ACS48 as promising lead compounds for future antileishmanial drug development. Full article
(This article belongs to the Special Issue Pharmacological Treatments for Parasitic Diseases)
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