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Special Issue "Antiparasitics 2023"

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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

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Research

21 pages, 3157 KiB

Open AccessArticle

Synthesis, Antimalarial, Antileishmanial, and Cytotoxicity Activities and Preliminary In Silico ADMET Studies of 2-(7-Chloroquinolin-4-ylamino)ethyl Benzoate Derivatives

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

and

Pharmaceuticals 2023, 16(12), 1709; https://doi.org/10.3390/ph16121709 (registering DOI) - 09 Dec 2023

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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 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

Open AccessCommunication

Design, Synthesis, and Repurposing of Rosmarinic Acid-β-Amino-α-Ketoamide Hybrids as Antileishmanial Agents

and

Pharmaceuticals 2023, 16(11), 1594; https://doi.org/10.3390/ph16111594 - 12 Nov 2023

Viewed by 472

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 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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