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Molecules
Special Issues
Development and Application of Anti-protozoan Agents
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Special Issue "Development and Application of Anti-protozoan Agents"

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

Deadline for manuscript submissions: closed (30 June 2020) | Viewed by 5352

Special Issue Editor

Prof. Dr. Yoichi Nakao

E-Mail Website
Guest Editor
Department of Chemistry and Biochemistry, Graduate School of Advanced Science and Engineering, Waseda University, Tokyo, Japan
Interests: chemical biology; marine natural products; functional food science; epigenetics; stem cell biology; (including all above words in a concept of) chemical epigenomics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

There are growing needs for the new anti-protozoan agents to treat the neglected tropical diseases (NTDs). So far, numbers of lead compounds have been discovered from natural sources, and some of them were successfully developed as anti-protozoan drugs. However, the emergence of resistance against existing drugs or unavailability of treatments for some of the NTDs still force us to search for new anti-protozoan drugs. With this situation in mind, in this Special Issue on “Development and Application of Anti-protozoan Agents”, we would like to get together for the development of new treatments against NTDs.

Prof. Dr. Yoichi Nakao
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. 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 2700 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

  • NTDs
  • anti-protozoan agents
  • natural products
  • synthetic compounds
  • SAR study
  • mode of action

Published Papers (1 paper)

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Research

15 pages, 5351 KiB  
Article
Metronidazole and Secnidazole Carbamates: Synthesis, Antiprotozoal Activity, and Molecular Dynamics Studies
by
Genaro Rocha-Garduño
,
Norma Angélica Hernández-Martínez
,
Blanca Colín-Lozano
,
Samuel Estrada-Soto
,
Emanuel Hernández-Núñez
,
Fernando Daniel Prieto-Martínez
,
José L. Medina-Franco
,
Juan Bautista Chale-Dzul
,
Rosa Moo-Puc
and
Gabriel Navarrete-Vázquez
Molecules 2020, 25(4), 793; https://doi.org/10.3390/molecules25040793 - 12 Feb 2020
Cited by 12 | Viewed by 5091
Abstract
We prepared a series of 10 carbamates derivatives based on two common antiprotozoal drugs: metronidazole (1–5) and secnidazole (6–10). The compounds were tested in vitro against a set of two amitochondriate protozoa: Giardia duodenalis and [...] Read more.
We prepared a series of 10 carbamates derivatives based on two common antiprotozoal drugs: metronidazole (1–5) and secnidazole (6–10). The compounds were tested in vitro against a set of two amitochondriate protozoa: Giardia duodenalis and Trichomonas vaginalis. Compounds 1–10 showed strong antiprotozoal activities, with potency values in the low micromolar-to-nanomolar range, being more active than their parent drugs. Metronidazole carbamate (1) was the most active of the series, with nanomolar activities against G. duodenalis (IC50 = 460 nM) and T. vaginalis (IC50 = 60 nM). The potency of compound 1 was 10 times greater than that of metronidazole against both parasites. None of compounds showed in vitro cytotoxicity against VERO cells tested at 100 µM. Molecular dynamics of compounds 1–10, secnidazole, and metronidazole onto the ligand binding site of pyruvate–ferredoxin oxidoreductase of T. vaginalis and the modeled β-tubulin of G. duodenalis revealed putative molecular interactions with key residues in the binding site of both proteins implicated in the mode of action of the parent drugs. Full article
(This article belongs to the Special Issue Development and Application of Anti-protozoan Agents)
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