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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 6701

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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
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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

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Keywords

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

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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 18 | Viewed by 6342
Abstract
We prepared a series of 10 carbamates derivatives based on two common antiprotozoal drugs: metronidazole (15) and secnidazole (610). 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 (15) and secnidazole (610). The compounds were tested in vitro against a set of two amitochondriate protozoa: Giardia duodenalis and Trichomonas vaginalis. Compounds 110 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 110, 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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