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Special Issue "Quinolones: Chemistry and Biological Activities"

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

Deadline for manuscript submissions: 20 April 2021.

Special Issue Editors

Prof. Dr. Giuseppe Manfroni
Website
Guest Editor
Department of Pharmaceutical Sciences, University of Perugia, 06123 Perugia, Italy
Interests: medicinal chemistry; drug design; molecular modeling; heterocyclic chemistry; organic synthesis; antivirals; antitumor agents; antibacterials; anti-inflammatory agents; chemical biology; kinase inhibitors; ionic liquids; enzyme inhibitors; nucleic acids binders; hit-to-lead optimization
Dr. Tommaso Felicetti
Website
Guest Editor
Università degli Studi di Perugia, Perugia, Italy
Interests: medicinal chemistry; drug design; molecular modeling; heterocyclic chemistry; organic synthesis; antimicrobial agents; antitumor agents; hit-to-lead optimization

Special Issue Information

Dear colleagues,

Quinolones represent a highly important class of synthetic antibacterial agents and received special attention in drug discovery. Developed in 1962, nalidixic acid, derived from chemical modifications of a by-product of the chloroquine synthesis, was the first quinolone approved for clinical use. Proper functionalization of the quinolone core can originate compounds endowed with a variety of biological activities including anticancer, antitubercular, antiviral, antimalarial, and anti-Alzheimer activities. Quinolones exert their antimicrobial activity by forming a ternary complex with DNA gyrase or Topoisomerase IV and bacterial DNA. In a similar manner, the anticancer activity is likely due to the formation of the ternary complex represented by quinolone/human Topoisomerase II/DNA.

In the last ten years, the two molecules vosaroxin and enoxacin have attracted much attention. Vosaroxin is currently in Phase III clinical trial as anticancer agent while enoxacin represents the first-in-class RNA interference enhancer molecule acting through the interaction with TAR-RNA binding protein, a co-factor involved in dicing activity of DICER. Beside the biological activities, the great importance of quinolones in the medicinal chemistry field has also driven the research towards the application of new and greener synthetic approaches.

In this special issue, we aim to collect a series of high-quality reviews and original papers spanning from chemical synthesis, drug repositioning of old quinolones, design of new molecules, analytical determination in the ecosystem, biological evaluation and last but not least toxicology aspects. We are proud to invite you to submit your own contribute on the special issue: “Quinolones: chemistry and biological activities”.

Prof. Giuseppe Manfroni
Dr. Tommaso Felicetti
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 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

  • Quinolone synthesis
  • Antimicrobial quinolones
  • Antitumor quinolones
  • Non-canonical activity of quinolones
  • Quinolones toxicity
  • Quinolone RNAi modulators
  • Quinolone in ecological environment
  • Quinolone resistance
  • Quinolones determination

Published Papers (2 papers)

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Research

Jump to: Review

Open AccessArticle
Quinolone and Organophosphorus Insecticide Residues in Bivalves and Their Associated Risks in Taiwan
Molecules 2020, 25(16), 3636; https://doi.org/10.3390/molecules25163636 - 10 Aug 2020
Abstract
Bivalves, such as freshwater clams (Corbicula fluminea) and hard clams (Meretrix lusoria), are the most extensive and widely grown shellfish in land-based ponds in Taiwan. However, few studies have examined the contamination of bivalves by quinolone and organophosphorus insecticides. [...] Read more.
Bivalves, such as freshwater clams (Corbicula fluminea) and hard clams (Meretrix lusoria), are the most extensive and widely grown shellfish in land-based ponds in Taiwan. However, few studies have examined the contamination of bivalves by quinolone and organophosphorus insecticides. Thus, we adapted an established procedure to analyze 8 quinolones and 12 organophosphorus insecticides using liquid and gas chromatography–tandem mass spectrometry. Surveys in Taiwan have not noted high residual levels of these chemicals in bivalve tissues. A total of 58 samples of freshwater or hard clams were obtained from Taiwanese aquafarms. We identified 0.03 mg/kg of enrofloxacin in one freshwater clam, 0.024 mg/kg of flumequine in one freshwater clam, 0.02 mg/kg of flumequine in one hard clam, 0.05 mg/kg of chlorpyrifos in one freshwater clam, 0.03 mg/kg of chlorpyrifos in one hard clam, and 0.02 mg/kg of trichlorfon in one hard clam. The results indicated that 5.17% of the samples had quinolone insecticide residues and 5.17% had organophosphorus residues. However, the estimated daily intake (EDI)/acceptable daily intake quotient (ADI) indicated no significant risk and no immediate health risk from the consumption of bivalves. These results provide a reference for the food-safety screening of veterinary drugs and pesticides in aquatic animals. Aquatic products should be frequently screened for residues of prohibited chemicals to safeguard human health. Full article
(This article belongs to the Special Issue Quinolones: Chemistry and Biological Activities)

Review

Jump to: Research

Open AccessReview
Quinolone Complexes with Lanthanide Ions: An Insight into their Analytical Applications and Biological Activity
Molecules 2020, 25(6), 1347; https://doi.org/10.3390/molecules25061347 - 16 Mar 2020
Cited by 1
Abstract
Quinolones comprise a series of synthetic bactericidal agents with a broad spectrum of activity and good bioavailability. An important feature of these molecules is their capacity to bind metal ions in complexes with relevant biological and analytical applications. Interestingly, lanthanide ions possess extremely [...] Read more.
Quinolones comprise a series of synthetic bactericidal agents with a broad spectrum of activity and good bioavailability. An important feature of these molecules is their capacity to bind metal ions in complexes with relevant biological and analytical applications. Interestingly, lanthanide ions possess extremely attractive properties that result from the behavior of the internal 4f electrons, behavior which is not lost upon ionization, nor after coordination. Subsequently, a more detailed discussion about metal complexes of quinolones with lanthanide ions in terms of chemical and biological properties is made. These complexes present a series of characteristics, such as narrow and highly structured emission bands; large gaps between absorption and emission wavelengths (Stokes shifts); and long excited-state lifetimes, which render them suitable for highly sensitive and selective analytical methods of quantitation. Moreover, quinolones have been widely prescribed in both human and animal treatments, which has led to an increase in their impact on the environment, and therefore to a growing interest in the development of new methods for their quantitative determination. Therefore, analytical applications for the quantitative determination of quinolones, lanthanide and miscellaneous ions and nucleic acids, along with other applications, are reviewed here. Full article
(This article belongs to the Special Issue Quinolones: Chemistry and Biological Activities)
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Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Planned paper 1:

Type of the paper: Review

Tentative title: Recent progress of in one-pot synthesis of quinolones 

Authors: Hee Nam Lim

Affiliations: Eco-Friendly New Materials Research Center, Therapeutics&Biotechnology Division, Korea Research Institute of Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, Republic of Korea

Planned paper 2:

Type of the paper: Article

Tentative title: Comparison of ecotoxicological effects of mixture of ciprofloxacin and enrofloxacin (active principle and commercial formulation) to Neotropical cladoceran

Authors: Silvina Vanesa Kergaravat

Affiliations: Laboratorio de Ecotoxicología (Facultad de Humanidades y Ciencias) / Laboratorio de Sensores y Biosensores (Facultad de Bioquímica y Ciencias Biológicas), Profesora Adjunta (Escuela Superior de Sanidad), Universidad Nacional del Litoral, Ciudad Universitaria CC242, CP S3000 - Santa Fe - Argentina

Tentative Abstract: The acute and chronic ecotoxicological effects to C. dubia of CIP and ENR -both active principle and commercial formulation- will be compared. Initially, the individual antibiotic (CIP or ENR) will be assayed and then, the mixture of CIP and ENR will be evaluated. The lethal concentrations 50 (LC50) obtained by acute ecotoxicity assay for each case will be compared, while survival, growth and reproduction will be the endpoint of life history traits analyzed in the chronic ecotoxicity assays. In addition, the quinolone stabilities –from active principle and commercial formulation- during the acute assays will be insured by the fluorometric method previously optimized. The interdisciplinary study will allowed knowing the behavior of two antibiotics to no target aquatic organisms.

Planned paper 3:

Type of the paper: Review

Tentative title: Biological effects of Quinolones: a family of broad-spectrum antibacterial agents broadly used

Authors: Alejandro A. Hidalgo

Affiliations: School of Pharmacy, Universidad Andrés Bello, Sazie 2320, Santiago, Chile

Planned paper 4:

Type of the paper: Article

Tentative title: Organophosphorus insecticide and quinolone residues in bivalves determined by liquid/gas chromatography–tandem mass spectrometry and their risk assessment

Authors: Geng-Ruei Chang

Affiliations: Division of Residual Control, Agricultural Chemicals and Toxic Substance Research Institute, Council of Agriculture, 11 Guangming Road, Wufeng, Taichung 41358, Taiwan, ROC Department of Veterinary Medicine, National Chiayi University, 580 Xinmin Road, Chiayi 60054, Taiwan, ROC Corresponding author at: Department of Veterinary Medicine, National Chiayi University, 580 Xinmin Road, Chiayi City, 60054, Taiwan

Title: Microbial alkylquinolones: discovery and biological properties
Authors: Muhammad Saalim and Benjamin R. Clark
Affiliation: Tianjin University
Abstract: The history of the alkylquinolones dates back to the 1960s, which saw the discovery of the first examples of this class of important secondary metabolites. They are characterized by a 4-quinolone nucleus, substituted at the 2- position by a variable group, most usually an alkyl moiety. Over the past decades, the number of reported examples has continued to increase, expanding the known structural motifs encountered. It is now known that the production of alkyl quinolones is not limited to the Pseudomonas genus, with examples reported from the Burkholderia, Pseudoalteromonas, and other genera. In recent decades it has been discovered that these metabolites are responsible for intercellular communication mediating quorum sensing behavior in many of the producing species, but they also possess significant pharmacological activity in a range of other areas, including antialgal, antimalarial, and anticancer properties. Here we review the discovery and structural diversity of this unique class of quinolones, and describe their biological properties, with a particular focus on their role in microbial communication.

Title: Optimization strategies aimed to increase the efficacy of Helicobacter pylori eradication therapies with quinolones
Authors: Javier P. Gisbert
Affiliation: Gastroenterology Unit, Hospital Universitario de La Princesa, Instituto de Investigación Sanitaria Princesa (IIS-IP), Universidad Autónoma de Madrid, Centro de Investigación Biomédica en Red de Enfermedades Hepáticas y Digestivas (CIBEREHD), Madrid, Spain

Title: Uptake of Ozenoxacin and other quinolones in Gram Positive bacteria
Authors: Jordi Vila
Affiliation: Department of Clinical Microbiology, Biomedical Diagnostic Center (CDB), Hospital Clinic School of Medicine, University of Barcelona, Barcelona, Spain

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