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Pharmaceuticals
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Antiparasitics 2023
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Antiparasitics 2023

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

Deadline for manuscript submissions: closed (29 February 2024) | Viewed by 2867

Special Issue Editor

Prof. Dr. Marcelo J. Nieto

E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, School of Pharmacy, Southern Illinois University Edwardsville, Edwardsville, IL 62026-2000, USA
Interests: drug design; parallel synthesis; anti-infective drugs; natural products; antivirals
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Parasitic infections affect more than two billion people worldwide and account for significant morbidity and mortality throughout the world. Antiparasitic drugs represent the main type of therapeutic treatment, but as is the case with most drugs, they have many side effects, and the risk of resistance is always a concern. Furthermore, the significant suffering and loss of productivity associated with these drugs results in a large financial burden for a population that already has limited resources. Many of the parasitic diseases are considered to be neglected tropical diseases (NTDs), as established by the World Health Organization (WHO). Most of the current antiparasitic drugs represent no financial return on investment for the pharmaceutical industry. Indeed, the development of new or novel antiparasitic drugs has been characterized by a lack of investment from the private sector and low attention from public health.

Despite the low financial return, there is a need for novel chemical entities with a new antiparasitic mechanism of action. In this Special Issue of Pharmaceuticals, we welcome both reviews and original research articles focused on the discovery and development of new antiparasitic drugs. The proposed topics include, but are not limited to, the following:

  • Validation of new targets;
  • New chemical entities with antiparasitic activity;
  • Natural products;
  • Novel strategies for the discovery and development of antiparasitic drugs;
  • Mechanism of resistance.

Prof. Dr. Marcelo J. Nieto
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

  • antiparasitic drugs
  • parasite resistance
  • small molecules
  • parasite
  • protozoa
  • helminth
  • drug discovery

Related Special Issue

Published Papers (3 papers)

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Research

18 pages, 9657 KiB  
Article
Global Health Priority Box: Discovering Flucofuron as a Promising Antikinetoplastid Compound
by Carlos J. Bethencourt-Estrella, Atteneri López-Arencibia, Jacob Lorenzo-Morales and José E. Piñero
Pharmaceuticals 2024, 17(5), 554; https://doi.org/10.3390/ph17050554 - 25 Apr 2024
Viewed by 287
Abstract
Leishmaniasis, produced by Leishmania spp., and Chagas disease, produced by Trypanosoma cruzi, affect millions of people around the world. The treatments for these pathologies are not entirely effective and produce some side effects. For these reasons, it is necessary to develop new [...] Read more.
Leishmaniasis, produced by Leishmania spp., and Chagas disease, produced by Trypanosoma cruzi, affect millions of people around the world. The treatments for these pathologies are not entirely effective and produce some side effects. For these reasons, it is necessary to develop new therapies that are more active and less toxic for patients. Some initiatives, such as the one carried out by the Medicines for Malaria Venture, allow for the screening of a large number of compounds of different origins to find alternatives to the lack of trypanocide treatments. In this work, 240 compounds were tested from the Global Health Priority Box (80 compounds with confirmed activity against drug-resistant malaria, 80 compounds for screening against neglected and zoonotic diseases and diseases at risk of drug resistance, and 80 compounds with activity against various vector species) against Trypanosoma cruzi and Leishmania amazonensis. Flucofuron, a compound with activity against vectors and with previous activity reported against Staphylococcus spp. and Schistosoma spp., demonstrates activity against L. amazonensis and T. cruzi and produces programmed cell death in the parasites. Flucofuron seems to be a good candidate for continuing study and proving its use as a trypanocidal agent. Full article
(This article belongs to the Special Issue Antiparasitics 2023)
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21 pages, 3157 KiB  
Article
Synthesis, Antimalarial, Antileishmanial, and Cytotoxicity Activities and Preliminary In Silico ADMET Studies of 2-(7-Chloroquinolin-4-ylamino)ethyl Benzoate Derivatives
by Joyce E. Gutiérrez, Hegira Ramírez, Esteban Fernandez-Moreira, María E. Acosta, Michael R. Mijares, Juan Bautista De Sanctis, Soňa Gurská, Petr Džubák, Marián Hajdúch, Liesangerli Labrador-Fagúndez, Bruno G. Stella, Luis José Díaz-Pérez, Gustavo Benaim and Jaime E. Charris
Pharmaceuticals 2023, 16(12), 1709; https://doi.org/10.3390/ph16121709 - 09 Dec 2023
Viewed by 1394
Abstract
A series of heterocyclic chloroquine hybrids, containing a chain of two carbon atoms at position four of the quinolinic chain and acting as a link between quinoline and several benzoyl groups, is synthesized and screened in vitro as an inhibitor of β-hematin formation [...] Read more.
A series of heterocyclic chloroquine hybrids, containing a chain of two carbon atoms at position four of the quinolinic chain and acting as a link between quinoline and several benzoyl groups, is synthesized and screened in vitro as an inhibitor of β-hematin formation and in vivo for its antimalarial activity against chloroquine-sensitive strains of Plasmodium berghei ANKA in this study. The compounds significantly reduced haeme crystallization, with IC50 values < 10 µM. The values were comparable to chloroquine’s, with an IC50 of 1.50 ± 0.01 µM. The compounds 4c and 4e prolonged the average survival time of the infected mice to 16.7 ± 2.16 and 14.4 ± 1.20 days, respectively. We also studied the effect of the compounds 4b, 4c, and 4e on another important human parasite, Leishmania mexicana, which is responsible for cutaneous leishmaniasis, demonstrating a potential leishmanicidal effect against promasigotes, with an IC50 < 10 µM. Concerning the possible mechanism of action of these compounds on Lesihmania mexicana, we performed experiments demonstrating that these three compounds could induce the collapse of the parasite mitochondrial electrochemical membrane potential (Δφ). The in vitro cytotoxicity assays against mammalian cancerous and noncancerous human cell lines showed that the studied compounds exhibit low cytotoxic effects. The ADME/Tox analysis predicted moderate lipophilicity values, low unbound fraction values, and a poor distribution for these compounds. Therefore, moderate bioavailability was expected. We calculated other molecular descriptors, such as the topological polar surface area, according to Veber’s rules, and except for 2 and 4i, the rest of the compounds violated this descriptor, demonstrating the low antimalarial activity of our compounds in vivo. Full article
(This article belongs to the Special Issue Antiparasitics 2023)
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13 pages, 3187 KiB  
Communication
Design, Synthesis, and Repurposing of Rosmarinic Acid-β-Amino-α-Ketoamide Hybrids as Antileishmanial Agents
by Ahmed H.E. Hassan, Waleed A. Bayoumi, Selwan M. El-Sayed, Trong-Nhat Phan, Taegeun Oh, Gyeongpyo Ham, Kazem Mahmoud, Joo Hwan No and Yong Sup Lee
Pharmaceuticals 2023, 16(11), 1594; https://doi.org/10.3390/ph16111594 - 12 Nov 2023
Cited by 1 | Viewed by 825
Abstract
A series of rosmarinic acid-β-amino-α-ketoamide hybrids were synthesized and rationally repurposed towards the identification of new antileishmanial hit compounds. Two hybrids, 2g and 2h, showed promising activity (IC50 values of 9.5 and 8.8 μM against Leishmania donovani promastigotes, respectively). Their activities were [...] Read more.
A series of rosmarinic acid-β-amino-α-ketoamide hybrids were synthesized and rationally repurposed towards the identification of new antileishmanial hit compounds. Two hybrids, 2g and 2h, showed promising activity (IC50 values of 9.5 and 8.8 μM against Leishmania donovani promastigotes, respectively). Their activities were comparable to erufosine. In addition, cytotoxicity evaluation employing human THP-1 cells revealed that the two hybrids 2g and 2h possess no cytotoxic effects up to 100 µM, while erufosine possessed cytotoxicity with CC50 value of 19.4 µM. In silico docking provided insights into structure–activity relationship emphasizing the importance of the aliphatic chain at the α-carbon of the cinnamoyl carbonyl group establishing favorable binding interactions with LdCALP and LARG in both hybrids 2g and 2h. In light of these findings, hybrids 2g and 2h are suggested as potential safe antileishmanial hit compounds for further development of anti-leishmanial agents. Full article
(This article belongs to the Special Issue Antiparasitics 2023)
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