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Pharmaceuticals
Special Issues
Platform Technologies and Emerging Modalities for Neglected Tropical Disease Therapeutics
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Platform Technologies and Emerging Modalities for Neglected Tropical Disease Therapeutics

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

Deadline for manuscript submissions: 30 June 2026 | Viewed by 2003

Special Issue Editors

Dr. Exequiel Porta

E-Mail Website
Guest Editor
UCL School of Pharmacy, University College London, London, UK
Interests: parasitology; neglected tropical diseases; infectious diseases; drug discovery; medicinal chemistry; chemical biology; bioinformatics; proteomics
Prof. Dr. Guillermo Labadie

E-Mail Website
Guest Editor
Rosario Chemistry Institute (IQUIR-CONICET), National University of Rosario, Rosario, Argentina
Interests: medicinal chemistry; organic chemistry; bioorganic chemistry; neglected tropical diseases
Dr. Brian Suárez Mantilla

E-Mail Website
Guest Editor
School of Chemistry, Faculty of Engineering and Physical Sciences, University of Leeds, Leeds, UK
Interests: microbiology; molecular parasitology; mass spectrometry; analytical biochemistry

Special Issue Information

Dear Colleagues,

Innovation in Neglected Tropical Disease (NTD) therapeutics is too often siloed by pathogen. This Special Issue overcomes this division by focusing on platform technologies and emerging modalities that accelerate discovery across NTDs. We spotlight approaches with cross-pathogen transferability—from trypanosomatids (leishmaniasis, Chagas disease, HAT) to viral (e.g., Dengue, Zika) and fungal pathogens—showcasing toolkits that move programmes from targets to candidates and toward translation.

We welcome original research articles and reviews on the following subjects: AI/ML-guided design, fragment-based discovery, covalent chemistry, PROTACs and molecular glues, chemoproteomics/activity-based protein profiling (ABPP), target deconvolution, and platform phenotypic→mechanism workflows. We are equally interested in emerging modalities beyond traditional small molecules, including peptides/peptidomimetics and biologics. Translational components (ADME/PK, PK/PD modelling, formulation and delivery, combination strategies, resistance/fitness mapping, and rigorous in vitro/in vivo efficacy) are also encouraged.

Submissions should articulate how approaches, targets, or chemotypes inform NTD therapeutics more broadly. Our goal is to catalyse cross-pollination between NTDs, showcasing platform concepts and toolkits that accelerate the development of clinically impactful therapies that improve global health.

Dr. Exequiel Porta
Prof. Dr. Guillermo Labadie
Dr. Brian Suárez Mantilla
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

  • neglected tropical diseases (NTDs)
  • leishmaniasis
  • Chagas disease
  • human African trypanosomiasis
  • Dengue
  • Zika
  • chikungunya
  • mycetoma
  • platform technologies
  • cross-pathogen therapeutics
  • drug discovery
  • medicinal chemistry
  • molecular targets
  • target deconvolution
  • new chemical entities
  • covalent inhibitors
  • peptides/peptidomimetics
  • biologics
  • structure-based design
  • AI/ML-guided design
  • phenotypic screening
  • hit-to-lead
  • lead optimisation
  • ADME/PK
  • PK/PD
  • formulation and delivery
  • resistance

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Published Papers (2 papers)

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Research

18 pages, 1911 KB  
Article
Mechanistic Exploration of N,N′-Disubstituted Diamines as Promising Chagas Disease Treatments
by Alejandro I. Recio-Balsells, Chantal Reigada, María Gabriela Mediavilla, Esteban Panozzo-Zénere, Miguel Villarreal Parra, Patricia S. Doyle, Juan C. Engel, Claudio A. Pereira, Julia A. Cricco and Guillermo R. Labadie
Pharmaceuticals 2026, 19(1), 119; https://doi.org/10.3390/ph19010119 - 9 Jan 2026
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Abstract
Introduction: Chagas disease, caused by the protozoan Trypanosoma cruzi, remains a major public health concern due to the limited effectiveness of current treatments, especially in the chronic stage. Objective: Here, we wanted to advance a library of 30 N,N′-disubstituted [...] Read more.
Introduction: Chagas disease, caused by the protozoan Trypanosoma cruzi, remains a major public health concern due to the limited effectiveness of current treatments, especially in the chronic stage. Objective: Here, we wanted to advance a library of 30 N,N′-disubstituted diamines as promising antichagasic agents and gain insight into the mechanism of action. Methods: The library was evaluated for activity against the T. cruzi amastigote stage and trypanocidal efficacy. In addition, selected compounds were tested as potential polyamine transport inhibitors, and a fluorescent analog was employed to investigate compound internalization. Results: Five compounds exhibited potent activity (pIC50 > 6.0), particularly those with short aliphatic linkers (3–6 carbon atoms), suggesting a structure–activity relationship favouring shorter chains. Mechanistic studies showed that compound 3c strongly inhibited polyamine transport, a vital pathway in T. cruzi, though this was not a universal mechanism among active hits, indicating the potential for multiple targets. A fluorescent analog confirmed intracellular uptake in amastigotes but lacked antiparasitic activity, likely due to disrupted pharmacophoric features. Importantly, none of the compounds demonstrated trypanocidal activity in long-term assays, and some showed cytotoxicity, particularly in the benzyloxy-substituted series. Conclusions: These findings position N,N′-disubstituted diamines as a viable scaffold for Chagas disease drug discovery. However, further optimization is required to enhance selectivity, achieve trypanocidal effects, and better understand the underlying mechanisms of action. Full article
(This article belongs to the Special Issue Platform Technologies and Emerging Modalities for Neglected Tropical Disease Therapeutics)
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25 pages, 1660 KB  
Article
Development of Novel Proline- and Pipecolic Acid-Based Allosteric Inhibitors of Dengue and Zika Virus NS2B/NS3 Protease
by Josè Starvaggi, Carla Di Chio, Johannes Lang, Valentina Belgiovine, Daniela Trisciuzzi, Santo Previti, Christian Klein, Orazio Nicolotti, Salvatore Di Maro, Maria Zappalà and Roberta Ettari
Pharmaceuticals 2026, 19(1), 24; https://doi.org/10.3390/ph19010024 - 22 Dec 2025
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Abstract
Background: In this study, we report a novel series of proline- and pipecolic acid-based small molecules designed as allosteric inhibitors of the NS2B/NS3 serine proteases from dengue and Zika viruses, key targets in antiviral drug discovery. Results: Enzymatic studies revealed that S-proline [...] Read more.
Background: In this study, we report a novel series of proline- and pipecolic acid-based small molecules designed as allosteric inhibitors of the NS2B/NS3 serine proteases from dengue and Zika viruses, key targets in antiviral drug discovery. Results: Enzymatic studies revealed that S-proline derivatives bearing electron-withdrawing substituents on the aromatic ring, particularly that with a trifluoromethyl group in meta position (i.e., compound 3, IC50 = 5.0 µM), were the most potent against DENV NS2B/NS3, while nitro-substituted inhibitors were mostly effective only against the ZIKV protease. R-configured pipecolic acid-based derivatives were the only ones active against DENV NS2B/NS3, even if the mid-micromolar range; however, they demonstrated improved cellular efficacy since inhibitors 24 and 27 exhibiting strong activity in a DENV2 protease reporter gene assay (EC50 = 5.2 and 5.1 µM, respectively). All compounds showed no cytotoxicity (CC50 > 100 µM) and were selective for the viral protease over off-target serine proteases. Structure-based approaches were exploited to map the druggable allosteric site close to Asn152. Conclusions: Our findings led us to identify proline and pipecolic acid-based inhibitors as promising leads for the development of selective flaviviral NS2B/NS3 allosteric inhibitors. Full article
(This article belongs to the Special Issue Platform Technologies and Emerging Modalities for Neglected Tropical Disease Therapeutics)
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