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Special Issue "Chalcone: A Privileged Structure in Medicinal Chemistry"

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

Deadline for manuscript submissions: 31 May 2018

Special Issue Editors

Guest Editor
Prof. Dr. Angela Rampa

Department of Pharmacy and Biotechnology, Alma Mater Studiorum—University of Bologna,Via Belmeloro 6, 40126 Bologna, Italy
Website | E-Mail
Interests: drug design; hybrid molecules; Alzheimer’s disease; AChE inhibitors; FAAH inhibitors; CB receptors ligands; flavonoids
Guest Editor
Prof. Dr. Alessandra Bisi

Department of Pharmacy and Biotechnology, Alma Mater Studiorum—University of Bologna,Via Belmeloro 6, 40126 Bologna, Italy
Website | E-Mail
Interests: flavonoids; hybrid molecules; privileged structures; MDR reversal; cytochromes P-450 inhibitors; Alzheimer’s disease

Special Issue Information

Dear Colleagues,

Chalcones belong to the flavonoid family and are widely distributed in edible plants. Naturally-occurring chalcones are endowed with a broad spectrum of biological activities and have been used in traditional medicine for many years. These natural products can be defined “privileged structures” and, as such, they can be properly exploited to develop effective strategies in drug discovery. The design and synthetic feasibility of chalcone-based compounds provides a new world of possibilities to find novel biological activities and unexplored therapeutic applications. Indeed, the peculiar electrophilic trans-α,β-unsaturated carbonyl framework of chalcone allows the molecule to interact with cysteine residues of different biological targets. Furthermore, because of their conjugated system, chalcones can be fluorescent, making them potential chemical probes for mechanistic investigations and imaging/diagnosis. This Special Issue aims to provide an overview of the latest applications of this intriguing class of natural/synthetic compounds in medicinal chemistry.

Prof. Dr. Angela Rampa
Prof. Dr. Alessandra Bisi
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 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 1800 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

  • chalcone
  • antioxidant
  • anticancer
  • anti-inflammatory
  • antibacterial
  • antimicrobial
  • neuroprotective effects
  • antimalarial
  • antidiabetic
  • Probes

Published Papers (1 paper)

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Research

Open AccessArticle Practical Synthesis of Chalcone Derivatives and Their Biological Activities
Molecules 2017, 22(11), 1872; doi:10.3390/molecules22111872
Received: 30 September 2017 / Revised: 21 October 2017 / Accepted: 24 October 2017 / Published: 1 November 2017
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Abstract
Practical synthesis and biological activities of 4-hydroxy-3-methoxy-2-propene derivatives are described. The novel chalcone derivatives were prepared by acid catalysed one-step condensation of 1,3- or 1,4-diacetylbenzene and 1,3,5-triacetylbenzene with 4-hydroxy-3-methoxybenzaldehyde. They were then evaluated for free radical scavenging activity, suppression of lipopolysaccharides (LPS)-induced NO
[...] Read more.
Practical synthesis and biological activities of 4-hydroxy-3-methoxy-2-propene derivatives are described. The novel chalcone derivatives were prepared by acid catalysed one-step condensation of 1,3- or 1,4-diacetylbenzene and 1,3,5-triacetylbenzene with 4-hydroxy-3-methoxybenzaldehyde. They were then evaluated for free radical scavenging activity, suppression of lipopolysaccharides (LPS)-induced NO generation, and anti-excitotoxicity in vitro. It was found that all compounds showed good effects for 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, LPS-induced NO generation, and anti-neurotoxicity. Compounds 6 and 7 were potent suppressor of NO generation with the concentration range 10 µM and especially compound 8 showed very potent anti-inflammatory activity with 1 µM. In addition, the di- and tri-acetylbenzyl derivatives 6, 7, and 8 showed enhanced anti-neurotoxicity activity in cultured cortical neurons. Molecular modelling studies to investigate the chemical structural characteristics required for the enhanced biological activities interestingly revealed that compound 8 has the smallest highest occupied molecular orbital-lowest energy unoccupied molecular orbital (HOMO-LUMO) gap, which signifies easy electron and radical transfer between HOMO and LUMO in model studies. Full article
(This article belongs to the Special Issue Chalcone: A Privileged Structure in Medicinal Chemistry)
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