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Microwave Assisted Reactions: A Modern Useful Tool in Medicinal Chemistry

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

Deadline for manuscript submissions: closed (31 December 2019) | Viewed by 8392

Special Issue Editor

Special Issue Information

Dear Colleagues,

Within the last few decades, microwave (MW)-assisted reactions have became a widely used and powerful tool method in medicinal and organic chemistry synthesis, offering some important advantages, such as significantly faster reaction times, milder conditions, increase in yield and selectivity, lower costs, and simplicity in handling and processing. Moreover, in recent years, combination with ultrasounds (US) seems to bring new advantages in terms of the synthetic approach. The demand of the pharmaceutical industry for new drugs with better activity and a lower cost make MW a useful alternative choice.

The aim of this Special Issue is to provide a platform to present the latest developments in microwave-assisted reactions in medicinal chemistry, focused on biological active heterocycle derivatives, especially (but not only) those one with anticancer, anti-HIV, antituberculosis, antimicrobial, etc. properties.

Prof. Dr. Ionel Mangalagiu
Guest Editor

Manuscript Submission Information

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Keywords

  • Microwave
  • Microwave and ultrasounds
  • Synthesis
  • Cycloadditions
  • Heterocycles
  • Anticancer
  • Antituberculosis
  • Antimicrobials
  • Anti-HIV
  • Other biological activities
  • Fluorescent derivatives for medicinal chemistry

Published Papers (3 papers)

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Research

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8 pages, 3360 KiB  
Article
Optimizing the Synthetic Route of Chromone-2-carboxylic Acids: A Step forward to Speed-up the Discovery of Chromone-based Multitarget-directed Ligands
by Fernando Cagide, Catarina Oliveira, Joana Reis and Fernanda Borges
Molecules 2019, 24(23), 4214; https://doi.org/10.3390/molecules24234214 - 20 Nov 2019
Cited by 4 | Viewed by 2990
Abstract
6-Bromochromone-2-carboxylic acid (3) was synthesized by a microwave-assisted process. The optimization of the reaction was performed varying parameters, such as type of base/number of reagent equivalents, solvent, temperature and reaction time. The yield of the reaction was improved to 87%. The [...] Read more.
6-Bromochromone-2-carboxylic acid (3) was synthesized by a microwave-assisted process. The optimization of the reaction was performed varying parameters, such as type of base/number of reagent equivalents, solvent, temperature and reaction time. The yield of the reaction was improved to 87%. The new synthetic route is versatile as several chromone-2-carboxylic acids (compounds 4B10B) were obtained with good yields (54–93%). Only in the case of the nitro substituent (compound 11B), an ester was obtained instead of the desired carboxylic acid. Following this synthetic route chromone carboxylic acids can be attained with a high degree of purity, without the need of the tedious and expensive purification processes through column chromatography. The reaction is safe, cost-effective, fast and robust, and can be used in the development of concise and diversity-oriented libraries based on chromone scaffold. The overall study can be looked as a step forward to speed-up the discovery of chromone-based multitarget-directed ligands. Full article
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11 pages, 1121 KiB  
Article
Microwave Assisted Reactions of Fluorescent Pyrrolodiazine Building Blocks
by Costel Moldoveanu, Dorina Amariucai-Mantu, Violeta Mangalagiu, Vasilichia Antoci, Dan Maftei, Ionel I. Mangalagiu and Gheorghita Zbancioc
Molecules 2019, 24(20), 3760; https://doi.org/10.3390/molecules24203760 - 18 Oct 2019
Cited by 14 | Viewed by 2241
Abstract
We report here the synthesis and optical spectral properties of several new pyrrolodiazine derivatives. The luminescent heterocycles were synthesized by 1,3-dipolar cycloaddition reactions between N-alkylated pyridazine and methylpropiolate or dimethyl acetylenedicarboxylate (DMAD). The pyrrolopyridazine derivatives are blue emitters with moderate quantum yields (around [...] Read more.
We report here the synthesis and optical spectral properties of several new pyrrolodiazine derivatives. The luminescent heterocycles were synthesized by 1,3-dipolar cycloaddition reactions between N-alkylated pyridazine and methylpropiolate or dimethyl acetylenedicarboxylate (DMAD). The pyrrolopyridazine derivatives are blue emitters with moderate quantum yields (around 25%) in the case of pyrrolopyridazines and negligible yet measurable emission for pyrrolophthalazines. In a subsequent step towards including the pyrrolodiazine moiety, given its spectral properties in various macromolecular frameworks such as biological molecules, a subset of the synthetized compounds has been subjected to α-bromination. A selective and efficient way for α-bromination in heterogeneous catalysis of pyrrolodiazine derivatives under microwave (MW) irradiation is presented. We report substantially higher yields under MW irradiation, whereas the solvent amounts required are at least five-fold less compared to classical heating. Full article
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Review

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20 pages, 7191 KiB  
Review
Microwave Assisted Reactions of Azaheterocycles Formedicinal Chemistry Applications
by Dorina Amariucai-Mantu, Violeta Mangalagiu, Ramona Danac and Ionel I. Mangalagiu
Molecules 2020, 25(3), 716; https://doi.org/10.3390/molecules25030716 - 07 Feb 2020
Cited by 22 | Viewed by 2789
Abstract
Microwave (MW) assisted reactions have became a powerful tool in azaheterocycles chemistry during the last decades. Five and six membered ring azaheterocycles are privileged scaffolds in modern medicinal chemistry possessing a large variety of biological activity. This review is focused on the recent [...] Read more.
Microwave (MW) assisted reactions have became a powerful tool in azaheterocycles chemistry during the last decades. Five and six membered ring azaheterocycles are privileged scaffolds in modern medicinal chemistry possessing a large variety of biological activity. This review is focused on the recent relevant advances in the MW assisted reactions applied to azaheterocyclic derivatives and their medicinal chemistry applications from the last five years. The review is divided according to the main series of azaheterocycles, more precisely 5- and 6-membered ring azaheterocycles (with one, two, and more heteroatoms) and their fused analogues. In each case, the reaction pathways, the advantages of using MW, and considerations concerning biological activity of the obtained products were briefly presented. Full article
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