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Special Issue "Emerging molecules for leishmaniasis therapy"

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (30 June 2021).

Special Issue Editors

Dr. Susana Santos Braga
E-Mail Website
Guest Editor
Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal
Interests: solid-solid reactions by mechanochemistry; cyclodextrin inclusion compounds; solubilisation of active pharmaceutical ingredients (APIs); local therapeutic systems for osteosarcoma and osteoporosis; antioxidant flavonoids and their Ru(II) complexes; natural and metallo-organic compounds for cytotoxic and biocidal activities; innovative medicines for leishmaniasis based on inorganic complexes and cyclodextrins
Special Issues and Collections in MDPI journals
Dr. Carlos J. P. Monteiro
E-Mail Website
Guest Editor
LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal
Interests: photodynamic therapy of cancer; organic synthesis of fine chemicals and pharmaceutical compounds; drug development; porphyrin and hydroporphyrin synthesis; photophysics and photochemistry of tetrapyrroles; near-infrared photosensitizers; water-soluble porphyrinoids and environmntal applications; dye-sensitized solar cells; biomedical applications of tetrapyrrolic macrocycles; translational research
Special Issues and Collections in MDPI journals
Dr. Carlos Silva
E-Mail Website
Guest Editor
LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal
Interests: Biochemistry; Organic Chemistry; Synthetic Chemistry; Heterocyclic Compounds (ex. Chromone, Quinoline and Acridine Derivatives); Biologically Active Compounds; Drug Design and Development; Multi-Target-Directed-Ligands (MTDLs); Neurodegenerative Diseases; Neglected Diseases; Leishmaniasis

Special Issue Information

Dear colleagues,

Leishmaniasis is a parasitic infection caused by various species of the Leishmania genus. Known to have affected humankind for thousands of years, leishmaniasis has typically remained endemic in warm climate areas of Africa, South America, India, and the Middle East. For its geographical distribution, and for the troubling short range of medicines avaialble to treat it, leishmaniasis was deemed as a Neglected Tropical Disease by the WHO. Presently, the disease is tending toward expansion, either due to global warming that is opening the doors for it to spread to Europe and North America, or due to increases in sociopolitical tension and civil war in Northern Africa and Middle-Eastern regions. As a response, the scientific community across the globe is intensifying efforts to find new active molecules against the disease. With this Special Issue, we are opening a forum for the presentation of the newest and most exciting results and perspectives on leishmanicidal drug design and discovery, from natural products to organic small molecules and metal complexes.

Dr. Susana Santos Braga
Dr. Carlos Monteiro
Dr. Carlos Silva
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 papers will be 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. Molecules is an international peer-reviewed open access semimonthly 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 2000 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 diseases
  • Protozoan parasite Leishmania
  • Drug design and discovery
  • Medicinal chemistry
  • Drug resistance
  • Multitarget compounds
  • Metal complexes
  • Photosensitisers
  • Natural products
  • Combination therapy
  • Photodynamic therapy

Published Papers (2 papers)

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Research

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Communication
Alkyl-Resorcinol Derivatives as Inhibitors of GDP-Mannose Pyrophosphorylase with Antileishmanial Activities
Molecules 2021, 26(6), 1551; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26061551 - 11 Mar 2021
Viewed by 811
Abstract
Leishmaniasis is a vector-borne disease caused by the protozoan parasite Leishmania found in tropical and sub-tropical areas, affecting 12 million people around the world. Only few treatments are available against this disease and all of them present issues of toxicity and/or resistance. In [...] Read more.
Leishmaniasis is a vector-borne disease caused by the protozoan parasite Leishmania found in tropical and sub-tropical areas, affecting 12 million people around the world. Only few treatments are available against this disease and all of them present issues of toxicity and/or resistance. In this context, the development of new antileishmanial drugs specifically directed against a therapeutic target appears to be a promising strategy. The GDP-Mannose Pyrophosphorylase (GDP-MP) has been previously shown to be an attractive therapeutic target in Leishmania. In this study, a chemical library of 5000 compounds was screened on both L. infantum (LiGDP-MP) and human (hGDP-MP) GDP-MPs. From this screening, oncostemonol D was found to be active on both GDP-MPs at the micromolar level. Ten alkyl-resorcinol derivatives, of which oncostemonols E and J (2 and 3) were described for the first time from nature, were then evaluated on both enzymes as well as on L. infantum axenic and intramacrophage amastigotes. From this evaluation, compounds 1 and 3 inhibited both GDP-MPs at the micromolar level, and compound 9 displayed a three-times lower IC50 on LiGDP-MP, at 11 µM, than on hGDP-MP. As they displayed mild activities on the parasite, these compounds need to be further pharmacomodulated in order to improve their affinity and specificity to the target as well as their antileishmanial activity. Full article
(This article belongs to the Special Issue Emerging molecules for leishmaniasis therapy)
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Review

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Review
Colombian Contributions Fighting Leishmaniasis: A Systematic Review on Antileishmanials Combined with Chemoinformatics Analysis
Molecules 2020, 25(23), 5704; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25235704 - 03 Dec 2020
Cited by 1 | Viewed by 1018
Abstract
Leishmaniasis is a parasitic morbid/fatal disease caused by Leishmania protozoa. Twelve million people worldwide are appraised to be currently infected, including ca. two million infections each year, and 350 million people in 88 countries are at risk of becoming infected. In Colombia, cutaneous [...] Read more.
Leishmaniasis is a parasitic morbid/fatal disease caused by Leishmania protozoa. Twelve million people worldwide are appraised to be currently infected, including ca. two million infections each year, and 350 million people in 88 countries are at risk of becoming infected. In Colombia, cutaneous leishmaniasis (CL) is a public health problem in some tropical areas. Therapeutics is based on traditional antileishmanial drugs, but this practice has several drawbacks for patients. Thus, the search for new antileishmanial agents is a serious need, but the lack of adequately funded research programs on drug discovery has hampered its progress. Some Colombian researchers have conducted different research projects focused on the assessment of the antileishmanial activity of naturally occurring and synthetic compounds against promastigotes and/or amastigotes. Results of such studies have separately demonstrated important hits and reasonable potential, but a holistic view of them is lacking. Hence, we present the outcome from a systematic review of the literature (under PRISMA guidelines) on those Colombian studies investigating antileishmanials during the last thirty-two years. In order to combine the general efforts aiming at finding a lead against Leishmania panamensis (one of the most studied and incident parasites in Colombia causing CL) and to recognize structural features of representative compounds, fingerprint-based analyses using conventional machine learning algorithms and clustering methods are shown. Abstraction from such a meta-description led to describe some function-determining molecular features and simplify the clustering of plausible isofunctional hits. This systematic review indicated that the Colombian efforts for the antileishmanials discovery are increasingly intensified, though improvements in the followed pathways must be definitively pursued. In this context, a brief discussion about scope, strengths and limitations of such advances and relationships is addressed. Full article
(This article belongs to the Special Issue Emerging molecules for leishmaniasis therapy)
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