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Special Issue "Antiparasitic Agents"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 May 2015)

Special Issue Editor

Guest Editor
Dr. Christophe Dardonville

1. Instituto de Química Médica – CSIC, Madrid, Spain
2. Medicinal Chemistry Institute – Spanish Council for Scientific Research
Website | E-Mail
Interests: medicinal chemistry, design and synthesis of antiparasitic agents for neglected tropical diseases (trypanosomiasis, leishmaniasis, malaria), cationic compounds, DNA binding study, pKa measurement

Special Issue Information

Dear Colleagues,

Parasitic diseases caused by protozoa and helminths represent a huge socioeconomic and life-threatening burden in less-developed countries. The World Health Organization reports that 11 out of 17 of the most neglected tropical diseases are caused by pathogenic parasites (http://www.who.int/neglected_diseases/diseases/en/). In recent years, a great effort has been made by the international scientific community to tackle this problem and discover new safe and effective drugs for these diseases. In this Special Issue, we would like to provide a picture of the recent discoveries in the field of antiparasitic agents for neglected tropical diseases and malaria.

We invite the submission of manuscripts covering the design, synthesis, in vitro/in vivo evaluation, and development of new antiparasitic molecules for the treatment of protozoan diseases and helminthiases. Review articles outlining recent developments in the field are also welcome.

Dr. Christophe Dardonville
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 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 1800 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

  • medicinal chemistry
  • antiparasitic drug synthesis
  • in vitro/in vivo activity
  • protozoa
  • helminths
  • neglected parasitic diseases
  • human African trypanosomiasis (sleeping sickness)
  • Chagas disease
  • leishmaniases
  • Dracunculiasis (guinea-worm disease)
  • Echinococcosis
  • Foodborne trematodiases
  • Lymphatic filariasis
  • Onchocerciasis (river blindness)
  • Schistosomiasis
  • Soil-transmitted helminthiases
  • malaria

Published Papers (5 papers)

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Research

Open AccessArticle 3-H-[1,2]Dithiole as a New Anti-Trypanosoma cruzi Chemotype: Biological and Mechanism of Action Studies
Molecules 2015, 20(8), 14595-14610; doi:10.3390/molecules200814595
Received: 29 May 2015 / Accepted: 7 August 2015 / Published: 12 August 2015
Cited by 8 | PDF Full-text (1011 KB) | HTML Full-text | XML Full-text
Abstract
The current pharmacological Chagas disease treatments, using Nifurtimox or Benznidazole, show limited therapeutic results and are associated with potential side effects, like mutagenicity. Using random screening we have identified new chemotypes that were able to inhibit relevant targets of the Trypanosoma cruzi.
[...] Read more.
The current pharmacological Chagas disease treatments, using Nifurtimox or Benznidazole, show limited therapeutic results and are associated with potential side effects, like mutagenicity. Using random screening we have identified new chemotypes that were able to inhibit relevant targets of the Trypanosoma cruzi. We found 3H-[1,2]dithioles with the ability to inhibit Trypanosoma cruzi triosephosphate isomerase (TcTIM). Herein, we studied the structural modifications of this chemotype to analyze the influence of volume, lipophilicity and electronic properties in the anti-T. cruzi activity. Their selectivity to parasites vs. mammalian cells was also examined. To get insights into a possible mechanism of action, the inhibition of the enzymatic activity of TcTIM and cruzipain, using the isolated enzymes, and the inhibition of membrane sterol biosynthesis and excreted metabolites, using the whole parasite, were achieved. We found that this structural framework is interesting for the generation of innovative drugs for the treatment of Chagas disease. Full article
(This article belongs to the Special Issue Antiparasitic Agents)
Figures

Open AccessArticle In Vitro Studies of Chromone-Tetrazoles against Pathogenic Protozoa, Bacteria, and Fungi
Molecules 2015, 20(7), 12436-12449; doi:10.3390/molecules200712436
Received: 29 May 2015 / Revised: 25 June 2015 / Accepted: 26 June 2015 / Published: 8 July 2015
Cited by 4 | PDF Full-text (1375 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
In vitro studies to fourteen previously synthesized chromone-tetrazoles and four novel fluorine-containing analogs were conducted against pathogenic protozoan (Entamoeba histolytica), pathogenic bacteria (Pseudomonas aeruginosa, and Staphylococcus aureus), and human fungal pathogens (Sporothrix schenckii, Candida albicans,
[...] Read more.
In vitro studies to fourteen previously synthesized chromone-tetrazoles and four novel fluorine-containing analogs were conducted against pathogenic protozoan (Entamoeba histolytica), pathogenic bacteria (Pseudomonas aeruginosa, and Staphylococcus aureus), and human fungal pathogens (Sporothrix schenckii, Candida albicans, and Candida tropicalis), which have become in a serious health problem, mainly in tropical countries. Full article
(This article belongs to the Special Issue Antiparasitic Agents)
Figures

Open AccessArticle Trypanocidal Activity of Long Chain Diamines and Aminoalcohols
Molecules 2015, 20(6), 11554-11568; doi:10.3390/molecules200611554
Received: 15 April 2015 / Revised: 16 June 2015 / Accepted: 17 June 2015 / Published: 23 June 2015
Cited by 3 | PDF Full-text (728 KB) | HTML Full-text | XML Full-text
Abstract
Thirteen aminoalcohols and eight diamines were obtained and tested against Trypanosoma cruzi epimastigotes strains MG, JEM and CL-B5 clone. Some of them were equal or more potent (1.0–6.6 times) than the reference compound nifurtimox. From them, three aminoalcohols and two diamines were selected
[...] Read more.
Thirteen aminoalcohols and eight diamines were obtained and tested against Trypanosoma cruzi epimastigotes strains MG, JEM and CL-B5 clone. Some of them were equal or more potent (1.0–6.6 times) than the reference compound nifurtimox. From them, three aminoalcohols and two diamines were selected for amastigotes assays. Compound 5 was as potent as the reference drug nifurtimox against amastigotes of the CL-B5 strain (IC50 = 0.6 µM), with a selectivity index of 54. Full article
(This article belongs to the Special Issue Antiparasitic Agents)
Open AccessArticle Potential Amoebicidal Activity of Hydrazone Derivatives: Synthesis, Characterization, Electrochemical Behavior, Theoretical Study and Evaluation of the Biological Activity
Molecules 2015, 20(6), 9929-9948; doi:10.3390/molecules20069929
Received: 18 March 2015 / Accepted: 24 April 2015 / Published: 29 May 2015
Cited by 5 | PDF Full-text (1908 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Four new hydrazones were synthesized by the condensation of the selected hydrazine and the appropriate nitrobenzaldehyde. A complete characterization was done employing 1H- and 13C-NMR, electrochemical techniques and theoretical studies. After the characterization and electrochemical analysis of each compound, amoebicidal activity
[...] Read more.
Four new hydrazones were synthesized by the condensation of the selected hydrazine and the appropriate nitrobenzaldehyde. A complete characterization was done employing 1H- and 13C-NMR, electrochemical techniques and theoretical studies. After the characterization and electrochemical analysis of each compound, amoebicidal activity was tested in vitro against the HM1:IMSS strain of Entamoeba histolytica. The results showed the influence of the nitrobenzene group and the hydrazone linkage on the amoebicidal activity. meta-Nitro substituted compound 2 presents a promising amoebicidal activity with an IC50 = 0.84 μM, which represents a 7-fold increase in cell growth inhibition potency with respect to metronidazole (IC50 = 6.3 μM). Compounds 1, 3, and 4 show decreased amoebicidal activity, with IC50 values of 7, 75 and 23 µM, respectively, as a function of the nitro group position on the aromatic ring. The observed differences in the biological activity could be explained not only by the redox potential of the molecules, but also by their capacity to participate in the formation of intra- and intermolecular hydrogen bonds. Redox potentials as well as the amoebicidal activity can be described with parameters obtained from the DFT analysis. Full article
(This article belongs to the Special Issue Antiparasitic Agents)
Figures

Open AccessArticle Toxicity of Fatty Acid Autoxidation Products: Highest Anti-Microbial Toxicity in the Initial Oxidative Phase
Molecules 2015, 20(1), 35-42; doi:10.3390/molecules20010035
Received: 17 November 2014 / Accepted: 15 December 2014 / Published: 23 December 2014
Cited by 1 | PDF Full-text (723 KB) | HTML Full-text | XML Full-text
Abstract
The autoxidation-degradation processes of polyunsaturated fatty acids give rise to toxic products, and the relative toxicity at different stages of the process is of great interest. We report here that when methyl α-linolenate is exposed to sunlight and air, its antimicrobial activity against
[...] Read more.
The autoxidation-degradation processes of polyunsaturated fatty acids give rise to toxic products, and the relative toxicity at different stages of the process is of great interest. We report here that when methyl α-linolenate is exposed to sunlight and air, its antimicrobial activity against yeasts and bacteria (as measured by agar diffusion) reaches its maximum during the early oxidative phase when addition of oxygen occurs and the mass increases drastically. Before exposure, the activity is minimal or zero, but it increases rapidly during the first days of the test, simultaneously with the increase of the mass of the material, and begins to decrease while the mass is still increasing and before the mass begins to decrease due to degradation and formation of volatile compounds. Thus, the products formed during the degradation phase of the process are far less toxic to the test organisms than the compounds formed at the early stages when addition of oxygen occurs with maximal rate. Full article
(This article belongs to the Special Issue Antiparasitic Agents)
Figures

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