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Pharmaceuticals
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Drug Discovery and Development for Parasitic Diseases
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Drug Discovery and Development 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 2025 | Viewed by 3174

Special Issue Editor

Dr. Francois Dufrasne

E-Mail Website
Guest Editor
Faculté de Pharmacie, Université Libre de Bruxelles, Campus Plaine CP 205/5, 1050 Brussels, Belgium
Interests: medicinal chemistry; organic synthesis; asymmetric synthesis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Following the Centre for Disease Control (CDC), a parasite is “an organism that lives on or in a host organism and gets its food from or at the expense of its host”. Parasites found in human diseases are protozoa, helminths (worms), and ectoparasites (an organism living outside living organisms such as mites or insects). In medicine history, these pathogens have been neglected. On the one hand, they were generally first described in Western countries, where they were not among one of the biggest threats for the population, while they were killing a lot of people in (sub)tropical regions. On the other hand, they have been overshadowed by other pathogens, such as bacteria, fungi, and viruses, who have become the most studied causes of pathogenic diseases since the beginning of the 20th century.

As a consequence, research stalled for decades, and only a few compounds can be seen as both significantly effective and safe for ill people. Among them, one can find quinine, artemisinin, and their derivatives against protozoa; ivermectin and benzimidazoles against worms; and pyrethrins against ectoparasites. Furthermore, the use of non-specific compounds such as insecticides to kill the parasites themselves or their vectors has poisoned both people and their environment, resulting in resistances. Resistance has also affected the drugs since they have been used for decades, and more efficacious molecules are greatly needed.

The following Special Issue aims to provide researchers with the opportunity to lay out the results of their investigations or their hypotheses to fight these overlooked diseases.

Dr. Francois Dufrasne
Guest Editor

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

  • parasitic diseases
  • biological activity
  • synthesis
  • pharmacology
  • medicine
  • chemistry
  • target

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Published Papers (4 papers)

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Research

14 pages, 719 KiB  
Article
Repositioning FDA-Approved Sulfonamide-Based Drugs as Potential Carbonic Anhydrase Inhibitors in Trypanosoma cruzi: Virtual Screening and In Vitro Studies
by Eyra Ortiz-Pérez, Adriana Moreno-Rodríguez, Timoteo Delgado-Maldonado, Jessica L. Ortega-Balleza, Alonzo González-González, Alma D. Paz-González, Karina Vázquez, Guadalupe Avalos-Navarro, Simone Giovannuzzi, Claudiu T. Supuran and Gildardo Rivera
Pharmaceuticals 2025, 18(5), 669; https://doi.org/10.3390/ph18050669 - 1 May 2025
Viewed by 311
Abstract
Background/Objectives: α-carbonic anhydrase (α-TcCA) has emerged as a promising drug target in T. cruzi, the causative agent of Chagas disease in the Americas. Sulfonamides, known inhibitors of CAs, bind to the zinc ion on the enzyme’s active site. This study proposes the [...] Read more.
Background/Objectives: α-carbonic anhydrase (α-TcCA) has emerged as a promising drug target in T. cruzi, the causative agent of Chagas disease in the Americas. Sulfonamides, known inhibitors of CAs, bind to the zinc ion on the enzyme’s active site. This study proposes the repositioning of sulfonamide-based drugs to identify new trypanocidal agents. Method: Ligand-based virtual screening and molecular docking analysis were performed on FDA-approved drugs targeting α-TcCA. These compounds were evaluated in vitro and ex vivo against the A1 and NINOA strains, followed by enzymatic assays. Results: Four sulfonylureas were selected: glimepiride (Glim), acetohexamide (Ace), gliclazide (Glic), and tolbutamide (Tol). Ace and Tol had half-maximal inhibitory concentration (IC50) values similar or better than reference drugs against the NINOA strain in the epimastigote and trypomastigote stages, while Glic and Glim had the highest activity against the A1 strain (epimastigotes and amastigotes). Notably, Ace had the highest trypanocidal activity against all stages in NINOA, with IC50 values of 6.5, 46.5, and 46 μM for epimastigotes, trypomastigotes, and amastigotes, respectively. Additionally, Ace inhibited α-TcCA with KI = 5.6 μM, suggesting that its trypanocidal effect is associated to the enzyme inhibition. Conclusions: This study supports the repositioning of FDA-approved sulfonamide-based hypoglycaemic agents as trypanocidal compounds. Future studies should focus on structural modifications to improve selectivity. Integrating docking, parasitological, and enzymatic data is crucial for optimizing drug candidates for Chagas disease. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Parasitic Diseases)
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14 pages, 4140 KiB  
Article
In Vitro Evaluation of Esters of Quinoxaline-1,4-di-N-oxide Derivatives as New Antitaeniasis Agents and Their Inhibitory Activity Against Triosephosphate Isomerase
by Francisca Palomares-Alonso, Alonzo González-González, Alma D. Paz-González, Eyra Ortiz-Pérez, Ana Verónica Martínez-Vázquez, Itzhel García-Torres, Gabriel López-Velázquez, Helgi Jung-Cook and Gildardo Rivera
Pharmaceuticals 2025, 18(3), 406; https://doi.org/10.3390/ph18030406 - 13 Mar 2025
Viewed by 549
Abstract
Background/Objectives: Pork tapeworm Taenia solium is the causative agent of cysticercosis which may develop in muscle tissue, skin, eyes, and the central nervous system (neurocysticercosis). It is estimated by the World Health Organization (WHO) that about 2.56–8.30 million are infected worldwide. Praziquantel and [...] Read more.
Background/Objectives: Pork tapeworm Taenia solium is the causative agent of cysticercosis which may develop in muscle tissue, skin, eyes, and the central nervous system (neurocysticercosis). It is estimated by the World Health Organization (WHO) that about 2.56–8.30 million are infected worldwide. Praziquantel and albendazole are used for anthelminthic treatment of neurocysticercosis; however, not all patients have a complete elimination of cysts, which makes it necessary to seek new and improved treatment options. Methods: In this study, methyl, ethyl, n-propyl, and iso-propyl quinoxaline-7-carboxylate-1,4-di-N-oxide derivatives were evaluated in vitro against Taenia crassiceps (T. crassiceps) cysts. Additionally, to know their potential mode of action, a molecular docking analysis on T. solium triosephosphate isomerase (TsTIM) and an enzyme inactivation assay on recombinant TsTIM were carried out. Results: Nine compounds had time- and concentration-dependent cysticidal activity. Particularly, compounds TS-12, TS-19, and TS-20 (EC50 values 0.58, 1.02, and 0.80 µM, respectively) were equipotent to albendazole sulfoxide (EC50 = 0.68 µM). However, TS-12 compounds only cause a slight inhibition of TsTIM (<40% at 1000 µM), suggested that another drug target is implicated in the biological effects. Conclusions: These results demonstrated that quinoxaline 1,4-di-N-oxide is a scaffold to develop new and more potent antitaeniasis agents, although it is necessary to explore other pharmacological targets to understand their mode of action. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Parasitic Diseases)
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11 pages, 453 KiB  
Article
Enhanced Anti-Babesia Efficacy of Buparvaquone and Imidocarb When Combined with ELQ-316 In Vitro Culture of Babesia bigemina
by Natalia M. Cardillo, Nicolas F. Villarino, Paul A. Lacy, Joseph S. Doggett, Michael K. Riscoe, Carlos E. Suarez, Massaro W. Ueti and Chungwon J. Chung
Pharmaceuticals 2025, 18(2), 218; https://doi.org/10.3390/ph18020218 - 6 Feb 2025
Viewed by 931
Abstract
Background/Objectives: B. bigemina is a highly pathogenic and widely distributed tick-borne disease parasite responsible for bovine babesiosis. The development of effective and safe therapies is urgently needed for global disease control. The aim of this study is to compare the effects of [...] Read more.
Background/Objectives: B. bigemina is a highly pathogenic and widely distributed tick-borne disease parasite responsible for bovine babesiosis. The development of effective and safe therapies is urgently needed for global disease control. The aim of this study is to compare the effects of endochin-like quinolone (ELQ-316), buparvaquone (BPQ), imidocarb (ID), and the combinations of ID + ELQ-316 and BPQ + ELQ-316, on in vitro survival of B. bigemina. Methods: Parasites at a starting parasitemia level of 2%, were incubated with each single drug and a combination of drugs, ranging from 25 to 1200 nM of concentration over four consecutive days. The inhibitory concentrations, 50% (IC50%) and 99% (IC99%), were estimated. Parasitemia levels were evaluated daily using microscopic examination. Data were statistically compared using the non-parametrical Kruskall–Wallis test. Results: All drugs tested significantly inhibited (p < 0.05) the growth of B. bigemina at 2% parasitemia. The combination of ID + ELQ-316 exhibited a lower mean (IC50%: 9.2; confidence interval 95%: 8.7–9.9) than ID (IC50%: 61.5; confidence interval 95%: 59.54–63.46), ELQ-316 (IC50%: 48.10; confidence interval 95%: 42.76–58.83), BPQ (IC50%: 44.66; confidence interval 95%: 43.56–45.81), and BPQ + ELQ-316 (IC50%: 27.59; confidence interval: N/A). Parasites were no longer viable in cultures treated with the BPQ + ELQ-316 combination, as well as with BPQ alone at a concentration of 1200 nM, on days 2 and 3 of treatment, respectively. Conclusions: BPQ and ID increase the babesiacidal effect of ELQ-316. The efficacy of these combinations deserves to be evaluated in vivo, which could lead to a promising and safer treatment option for B. bigemina. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Parasitic Diseases)
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14 pages, 1529 KiB  
Article
Repurposing the Antidiabetic Drugs Glyburide, Gliquidone, and Glipizide in Combination with Benznidazole for Trypanosoma cruzi Infection
by Citlali Vázquez, Rusely Encalada, Isabel Jiménez-Galicia, Rogelio Gómez-Escobedo, Gildardo Rivera, Benjamín Nogueda-Torres and Emma Saavedra
Pharmaceuticals 2025, 18(1), 21; https://doi.org/10.3390/ph18010021 - 27 Dec 2024
Viewed by 929
Abstract
Infection with the protozoan parasite Trypanosoma cruzi causes human Chagas disease. Benznidazole (BNZ) and nifurtimox are the current drugs for the treatment; however, they induce severe adverse side effects in patients; therefore, there is a need to improve the treatment effectiveness and efficiency [...] Read more.
Infection with the protozoan parasite Trypanosoma cruzi causes human Chagas disease. Benznidazole (BNZ) and nifurtimox are the current drugs for the treatment; however, they induce severe adverse side effects in patients; therefore, there is a need to improve the treatment effectiveness and efficiency of these drugs for its safer use. Background/Objective: Glyburide, glipizide, and gliquidone, hypoglycemic drugs for diabetes treatment, were previously predicted to bind to dihydrofolate reductase-thymidylate synthase from T. cruzi by in silico docking analysis; they also showed antiproliferative effects against T. cruzi epimastigotes, the stage of the insect vector. In the present study, the potential parasiticidal effect of these antidiabetic drugs was tested in monotherapy and bi-therapy with BNZ in human cells in vitro and in animals. Methods: Evaluation was performed in (a) a model of in vitro infection of T. cruzi trypomastigotes using human fibroblasts as host cells and (b) in mice infected with T. cruzi. Results: The antidiabetic drugs in monotherapy showed antiparasitic effects in preventing infection progression (trypomastigotes release), with an IC50 of 8.4–14.3 µM in comparison to that of BNZ (0.26 µM) in vitro. However, in bi-therapy, the presence of just 0.5 or 1 µM of the antidiabetics decreased the BNZ IC50 by 5–10 times to 0.03–0.05 µM. Remarkably, the antidiabetic drugs in monotherapy decreased the infection in mice by 40–60% in a similar extent to BNZ (80%). In addition, the combination of BNZ plus antidiabetics perturbed the antioxidant metabolites in epimastigotes. Conclusions: These results identified antidiabetics as potential drugs in combination therapy with BNZ to treat T. cruzi infection. Full article
(This article belongs to the Special Issue Drug Discovery and Development for Parasitic Diseases)
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