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Special Issue "Biologically Active Small Molecules Inspired by Plant Secondary Metabolites"

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

Deadline for manuscript submissions: 31 December 2020.

Special Issue Editors

Assoc. Prof. Giovanni Lentini
Website
Guest Editor
University of Studies of Bari Aldo Moro, Bari, Italy
Interests: medicinal chemistry; drug discovery; chirality; pharmacology; phytochemistry
Special Issues and Collections in MDPI journals
Dr. Maria Maddalena Cavalluzzi
Website
Guest Editor
University of Studies of Bari Aldo Moro, Bari, Italy
Interests: organic synthesis; medicinal and pharmaceutical chemistry; small molecule synthesis; multistep synthesis; enantiomer; fluorine chemistry; sodium channels

Special Issue Information

Dear Colleagues,

It would seem that more than 500 centuries ago, our closest human relatives―the Neanderthals―used to place Ephedra plant flowers into graves. This might be the most ancient example of paleoethnobotany. As questionable as this statement might be, undoubtedly, the Plant Kingdom has been the most prodigal source of medicines for over 20 centuries.

The last four decades have witnessed a resurgence of interest in plant product research. Numerous and varied are the reasons for this:

  • Ever-increasing difficulty in developing new drugs;
  • The success of the natural product approach;
  • The uniqueness of plant secondary metabolites;
  • The impact of new screening methods and analytic techniques.

Unfortunately, plant secondary metabolites are not necessarily the best compounds for pharmaceutical uses, for the following reasons:

  • Limitations may exist that prevent the acquisition of sufficient biomass;
  • Isolation procedures may be long and expensive;
  • The structure of the secondary metabolites may be too complex to allow total synthesis;
  • The pharmacological profile may be promiscuous;
  • Toxicological aspects may cause concern;
  • Oral bioavailability can be too low.

For all of the above reasons, medicinal chemists use to prepare analogues of the starting secondary metabolites in order to unveil sound structure–activity relationships (SAR) and possibly overcome the above limitations.

This Special Issue is designed to scrutinize recent developments in the medicinal chemistry of biologically relevant compounds that were inspired by plant-derived compounds.

Between 1980 and 2013, 20% of the new drugs introduced into the market were either natural products or natural products derivatives, with the latter being highly predominant (18%). The contribution of natural product derivatives to the physician panoply is expected to rise in the next decade. The colleagues that would like to share their valuable work in the field by contributing to this Special Issue of Molecules will give shine to the issue, of course, and would possibly confer higher chances to this prophecy.

Assoc. Prof. Giovanni Lentini
Dr. Maria Maddalena Cavalluzzi
Prof. Solomon Habtemariam
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

  • Drug discovery
  • Secondary metabolites
  • Natural product scaffolds
  • Structure–activity relationships
  • Pharmacophore

Published Papers (2 papers)

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Open AccessFeature PaperArticle
Synthesis and In Vitro Growth Inhibition of 2-Allylphenol Derivatives Against Phythopthora cinnamomi Rands
Molecules 2019, 24(22), 4196; https://doi.org/10.3390/molecules24224196 - 19 Nov 2019
Cited by 1
Abstract
Phytophthora cinnamomi is a phytopathogen that causes extensive damage in different crops, and therefore, produces important economic losses all around the world. Chemical fungicides are a key factor for the control of this disease. However, ecological and environmental considerations, as well as the [...] Read more.
Phytophthora cinnamomi is a phytopathogen that causes extensive damage in different crops, and therefore, produces important economic losses all around the world. Chemical fungicides are a key factor for the control of this disease. However, ecological and environmental considerations, as well as the appearance of strains that are resistant to commercial fungicides, have prompted the quest for new antifungal agents which are of low ecological impact. In this work, a series of new 2-allylphenol derivatives was synthesized, and their structures were confirmed by FT-IR, NMR, and MS. Some of the synthesized compounds, more specifically nitro derivatives, exhibit strong growth inhibition of P. cinnamomi with EC50 as low as 10.0 µg/mL. This level of activity is similar to that exhibited by METALAXYL MZ 58 WP, a commonly-used commercial fungicide; therefore, these compounds might be of agricultural interest due to their potential use as fungicides against P. cinnamomi. The results indicate that this activity depends on the chemical structures of the 2-allylphenol derivatives, and that it is strongly enhanced in molecules where nitro and hydroxyl groups adopt a -para configuration. These effects are discussed in terms of the electronic distribution of the aromatic ring induced by substituent groups. Full article
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Open AccessCommentary
COVID-19, Chloroquine Repurposing, and Cardiac Safety Concern: Chirality Might Help
Molecules 2020, 25(8), 1834; https://doi.org/10.3390/molecules25081834 - 16 Apr 2020
Abstract
The desperate need to find drugs for COVID-19 has indicated repurposing strategies as our quickest way to obtain efficacious medicines. One of the options under investigation is the old antimalarial drug, chloroquine, and its analog, hydroxychloroquine. Developed as synthetic succedanea of cinchona alkaloids, [...] Read more.
The desperate need to find drugs for COVID-19 has indicated repurposing strategies as our quickest way to obtain efficacious medicines. One of the options under investigation is the old antimalarial drug, chloroquine, and its analog, hydroxychloroquine. Developed as synthetic succedanea of cinchona alkaloids, these chiral antimalarials are currently in use as the racemate. Besides the ethical concern related to accelerated large-scale clinical trials of drugs with unproven efficacy, the known potential detrimental cardiac effects of these drugs should also be considered. In principle, the safety profile might be ameliorated by using chloroquine/hydroxychloroquine single enantiomers in place of the racemate. Full article
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