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Special Issue "Application of Organic Synthesis to Bioactive Compounds"

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

Deadline for manuscript submissions: 30 June 2019

Special Issue Editors

Guest Editor
Prof. David Díez

Department of Organic Chemistry, Universidad de Salamanca, Castilla y León, Salamanca 37008, Spain
Website | E-Mail
Phone: 0034923294500
Interests: Natural product transformations; organocatalysis; organic synthesis
Guest Editor
Prof. María Ángeles Castro

Department of Pharmaceutical Sciences, Pharmaceutical Chemistry Section, CIETUS/IBSAL, Faculty of Pharmacy, University of Salamanca, Salamanca, Spain
Website | E-Mail
Interests: Natural product transformations; hybridation; anticancer and anti-parasitic compounds

Special Issue Information

Dear Colleagues,

After a billion of years of evolution, nature has achieved an enormous variety of chemical compounds that have extraordinary structural diversity and functional value. Many of these compounds have been used for plants and animals, for communication, relationships, etc. Humans have also realized that some of these compounds could be useful for the treatment of illnesses that affect their health. In many cases, the quantities available in nature are not enough for the treatment of affected people or even for appropriate biological testing. This makes it necessary to obtain them by other procedures. In this case, it is necessary to establish adequate starting materials for the synthesis not only of those biologically active compounds but also of their analogues. An easy approach is the structural manipulation of other abundant natural products to produce a similar functionalization to the bioactive compounds, which is known as hemi- or semi-synthesis. Other approaches include total synthesis. Recently there has been a large variety of methodologies directed at achieving bioactive compounds, such as diversity-oriented synthesis, target-oriented synthesis, biologically-oriented synthesis, and function-oriented synthesis, among others.

The Special Issue “Application of Organic Synthesis to Bioactive Compounds” aims to present the most recent achievements in the organic synthesis not only of natural products, but also the synthesis of active compounds not present in nature. The manuscripts together with review papers will summarize the “state of the art” of the synthesis of bioactive compounds.

Prof. David Díez
Prof. María Ángeles Castro
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 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

  • Natural products
  • Organic synthesis
  • Bioactive compounds

Published Papers (3 papers)

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Research

Open AccessArticle A Straightforward Synthesis of Functionalized cis-Perhydroisoquinolin-1-ones
Molecules 2019, 24(3), 557; https://doi.org/10.3390/molecules24030557
Received: 15 January 2019 / Revised: 29 January 2019 / Accepted: 30 January 2019 / Published: 3 February 2019
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Abstract
Base-catalyzed annulation reactions of 5,6-dihydro-2(1H)-pyridones with Nazarov-type reagents are reported. The effect of the solvent polarity and the concentration of the reagents is studied. The process involves two successive Michael additions and stereoselectively provides functionalized cis-perhydroisoquinolin-1-ones. Full article
(This article belongs to the Special Issue Application of Organic Synthesis to Bioactive Compounds)
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Open AccessArticle Comparison of the Inhibitory Activities of 5,6-Dihydroergosterol Glycoside α- and β-Anomers on Skin Inflammation
Molecules 2019, 24(2), 371; https://doi.org/10.3390/molecules24020371
Received: 5 December 2018 / Revised: 12 January 2019 / Accepted: 19 January 2019 / Published: 21 January 2019
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Abstract
Chronic skin inflammatory diseases, such as atopic dermatitis, are associated with a dysfunctional skin barrier due to an increase in various inflammatory stimuli, for instance inflammatory cytokines and chemokines. In particular, CCL17 and CCL22 expression is increased in patients with chronic skin inflammation. [...] Read more.
Chronic skin inflammatory diseases, such as atopic dermatitis, are associated with a dysfunctional skin barrier due to an increase in various inflammatory stimuli, for instance inflammatory cytokines and chemokines. In particular, CCL17 and CCL22 expression is increased in patients with chronic skin inflammation. In this study, we synthesized several α- and β-anomers of dihydroergosterol (DHE)-glycosides and assessed their effects on CCL17 and CCL22 expression. We confirmed that the β-anomers of DHE-glycosides were superior to α-anomers of DHE-glycosides in inhibiting CCL17 and CCL22 mRNA and protein expression. In addition, we determined that DHE-glycoside β-anomers showed strong inhibitory activity towards pro-inflammatory cytokine mRNA and protein expression, including that of TNF-α, IL-6, and IL-1β- in stimulated HaCaT cells. These results imply that DHE-glycoside α- and β-anomers should be separated during synthesis of drugs for chronic skin inflammation. Our results also suggest that β-anomers of DHE-glycosides may play an important role as new drugs for chronic skin inflammation because of their ability to inhibit the skin inflammatory biomarker proteins CCL17 and CCL22. Full article
(This article belongs to the Special Issue Application of Organic Synthesis to Bioactive Compounds)
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Figure 1

Open AccessCommunication Synthesis, Anticancer Activity, and Apoptosis Induction of Novel 3,6-Diazaphenothiazines
Molecules 2019, 24(2), 267; https://doi.org/10.3390/molecules24020267
Received: 30 November 2018 / Revised: 9 January 2019 / Accepted: 9 January 2019 / Published: 12 January 2019
PDF Full-text (621 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
New 10-substituted derivatives of 3,6-diazaphenothiazine, containing the triple bond linker terminated with tertiary cyclic and acyclic amine groups, were synthesized and screened for their anticancer action. The compounds exhibited varied anticancer activities against human glioblastoma SNB-19, melanoma C-32, and breast cancer MDA-MB231 cell [...] Read more.
New 10-substituted derivatives of 3,6-diazaphenothiazine, containing the triple bond linker terminated with tertiary cyclic and acyclic amine groups, were synthesized and screened for their anticancer action. The compounds exhibited varied anticancer activities against human glioblastoma SNB-19, melanoma C-32, and breast cancer MDA-MB231 cell lines, depending on the nature of the substituents. The most active 3,6-diazaphenothiazine, 4, was the derivative with the N,N-diethylamino-2-butynyl substituent against glioblastoma SNB-19, and was ten times more potent than cisplatin. For this compound, the expression of H3, TP53, CDKN1A, BCL-2, and BAX genes was detected by the RT-qPCR method. The gene expression ratio BAX/BCL-2 indicated the induction of mitochondrial apoptosis in cancer cell lines. The transformation of the propynyl substituent into amino-2-butynyl can be a method applicable to the search for more anticancer-active azaphenothiazines. Full article
(This article belongs to the Special Issue Application of Organic Synthesis to Bioactive Compounds)
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Graphical abstract

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