Antibiotics

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Special Issue Information

Dear Colleagues,

The first volume of the Special Issue “Antimicrobial Activity of Plant-Derived Products and Synthetic Derivatives” was published in 2022. As it was a successful issue with twenty-two published papers, the editorial team encouraged us to introduce a second volume with the same topic.

This second volume intends to collect cutting-edge research and review works illustrating the potential of extracts and active principles obtained from plants, as well as their derivatives effective against microorganisms, with special attention to those with resistant phenotypes. It also aims to bring together pharmacognosists, chemists, pharmacologists, toxicologists, biologists, computer-aided drug design scientists and clinicians as a multidisciplinary team in the area of natural product use against pathogenic microorganisms.

Prof. Dr. Constantinos Athanassopoulos
Prof. Dr. María Cecilia Carpinella
Prof. Dr. Carlos L. Cespedes-Acuña
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 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. Antibiotics 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.

Related Special Issue

Published Papers (1 paper)

Research

22 pages, 1460 KiB

Open AccessArticle

Synthesis of Novel Artemisinin, Ciprofloxacin, and Norfloxacin Hybrids with Potent Antiplasmodial Activity

by Georgia Vamvoukaki, Antonia I. Antoniou, Michel Baltas, Elisabeth Mouray, Sebastien Charneau, Philippe Grellier and Constantinos M. Athanassopoulos

Antibiotics 2024, 13(2), 142; https://doi.org/10.3390/antibiotics13020142 - 01 Feb 2024

Viewed by 992

Abstract

The synthesis and antiplasmodial evaluation of new hybrids combining the pharmacophore structures of artemisinin, ciprofloxacin or norfloxacin, and 7-chloroquinoline are reported in this study. The first step for all of the syntheses is the obtainment of key piperazine esters intermediates bearing the drugs ciprofloxacin and norfloxacin. Using these platforms, 18 final compounds were synthesized through a multistep procedure with overall yields ranging between 8 and 20%. All compounds were screened for their antiplasmodial activity against the chloroquine-resistant Plasmodium falciparum FcB1 strain. Compounds 20, 21, 22, and 28, bearing an artesunate fragment with ciprofloxacin, exhibited IC₅₀ values in the range of 3.5–5.4 nM and excellent selectivity indices. Among the compounds bearing the artesunate moiety on the norfloxacin, two of them, 23 and 24, afforded IC₅₀ values of 1.5 nM and 1.9 nM, respectively. They also showed excellent selectivity indices. The most potent compounds were also evaluated against the CQ-resistant Dd2 strain of Plasmodium falciparum, demonstrating that those compounds incorporating the artesunate fragment were the most potent. Finally, the combination of artesunate with either ciprofloxacin or norfloxacin moieties in a single molecular entity proved to substantially enhance the activity and selectivity when compared to the administration of the unconjugated counterparts artesunate/ciprofloxacin and artesunate/norfloxacin. Full article

(This article belongs to the Special Issue Antimicrobial Activity of Plant-Derived Products and Synthetic Derivatives, 2nd Edition)

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