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Sustainable Chemistry in the Organic Synthesis of Bioactive Compounds

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

Deadline for manuscript submissions: closed (15 November 2023) | Viewed by 8012

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Special Issue Editors

Dr. Paola Costanzo

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Department of Chemistry and Chemical Technologies, University of Calabria, 87036 Arcavacata, Italy
Interests: green chemistry; MW-assisted reactions; biorenewable feedstocks; organic-synthesis; green solvents
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Antonio De Nino

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Guest Editor

Department of Chemistry and Chemical Technologies, University of Calabria, 87036 Rende, Italy
Interests: green chemistry; homogeneous catalysis; lanthanide Lewis acid catalysis; non-conventional reaction media; organic synthesis; asymmetric synthesis; composite material

Dr. Loredana Maiuolo

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Guest Editor

Department of Chemistry and Chemical Technologies, University of Calabria, Via P. Bucci, Cubo 12C, 87036 Rende, Italy
Interests: green chemistry; homogeneous catalysis; lanthanide Lewis acid catalysis; nonconventional reaction media; organic synthesis; asymmetric synthesis; MW-assisted chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Sustainable development is the new goal of modern society, for achieving “a healthy and productive life in harmony with Nature”. Chemistry plays a pivotal role in maintaining and improving our quality of life, the competitiveness of the chemical industry, and the natural environment. Starting from this, the twelve principles of green chemistry serve as excellent guidance when considering the environmental impact of any chemistry. Among them, the integration of green chemistry and engineering principles into the pharmaceutical industry is encouraged. With this aim, a wider pool of clean technologies could be customized for the synthesis of key molecules with biological activity. This Special Issue welcomes original research on the development of ecofriendly processes useful not only for organic synthesis but especially for medicinal chemistry. The scope is broad and includes (1) the use of renewable feedstocks, (2) the employment of alternative energy sources, (3) the use of non-toxic solvents, (4) catalysis, and (5) hazard reduction and waste minimization

Dr. Paola Costanzo
Prof. Dr. Antonio De Nino
Prof. Dr. Loredana Maiuolo
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 submissions that pass pre-check are 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 2700 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

Green chemistry
Biomasses
Renewable sources
Atom economy
Alternative reaction media
Solvent-free reaction
Medicinal chemistry
Bioactive compounds.

Published Papers (3 papers)

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Research

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18 pages, 9761 KiB

Open AccessArticle

Green Synthesis of Oxoquinoline-1(2H)-Carboxamide as Antiproliferative and Antioxidant Agents: An Experimental and In-Silico Approach to High Altitude Related Disorders

by Amena Ali, Abuzer Ali, Musarrat Husain Warsi, Mohammad Akhlaquer Rahman, Mohamed Jawed Ahsan and Faizul Azam

Molecules 2022, 27(1), 309; https://doi.org/10.3390/molecules27010309 - 04 Jan 2022

Cited by 1 | Viewed by 2063

Abstract

At high altitudes, drops in oxygen concentration result in the creation of reactive oxygen and nitrogen species (RONS), which cause a variety of health concerns. We addressed these health concerns and reported the synthesis, characterization, and biological activities of a series of 10 oxoquinolines. N-Aryl-7-hydroxy-4-methyl-2-oxoquinoline-1(2H)carboxamides (5a–j) were accessed in two steps under ultrasonicated irradiation, as per the reported method. The anticancer activity was tested at 10 µM against a total of 5 dozen cancer cell lines obtained from nine distinct panels, as per the National Cancer Institute (NCI US) protocol. The compounds 5a (TK-10 (renal cancer); %GI = 82.90) and 5j (CCRF-CEM (Leukemia); %GI = 58.61) showed the most promising anticancer activity. Compound 5a also demonstrated promising DPPH free radical scavenging activity with an IC₅₀ value of 14.16 ± 0.42 µM. The epidermal growth factor receptor (EGFR) and carbonic anhydrase (CA), two prospective cancer inhibitor targets, were used in the molecular docking studies. Molecular docking studies of ligand 5a (docking score = −8.839) against the active site of EGFR revealed two H-bond interactions with the residues Asp855 and Thr854, whereas ligand 5a (docking = −5.337) interacted with three H-bond with the residues Gln92, Gln67, and Thr200 against the active site CA. The reported compounds exhibited significant anticancer and antioxidant activities, as well as displayed significant inhibition against cancer targets, EGFR and CA, in the molecular docking studies. The current discovery may aid in the development of novel compounds for the treatment of cancer and oxidative stress, and other high altitude-related disorders. Full article

(This article belongs to the Special Issue Sustainable Chemistry in the Organic Synthesis of Bioactive Compounds)

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9 pages, 1791 KiB

Open AccessArticle

Structure–Activity Relationship Assessment of Sophorolipid Ester Derivatives against Model Bacteria Strains

by Filbert Totsingan, Fei Liu and Richard A. Gross

Molecules 2021, 26(10), 3021; https://doi.org/10.3390/molecules26103021 - 19 May 2021

Cited by 13 | Viewed by 2182

Abstract

Sophorolipids (SLs) are glycolipids that consist of a hydrophilic sophorose head group covalently linked to a hydrophobic fatty acid tail. They are produced by fermentation of non-pathogenic yeasts such as Candida Bombicola. The fermentation products predominantly consist of the diacetylated lactonic form that coexists with the open-chain acidic form. A systematic series of modified SLs were prepared by ring opening of natural lactonic SL with n-alkanols of varying chain length under alkaline conditions and lipase-selective acetylation of sophorose primary hydroxyl groups. The antimicrobial activity of modified SLs against Gram-positive human pathogens was a function of the n-alkanol length, as well as the degree of sophorose acetylation at the primary hydroxyl sites. Modified SLs were identified with promising antimicrobial activities against Gram-positive human pathogens with moderate selectivity (therapeutic index, TI = EC₅₀/MIC_{B. cereus} = 6–33). SL-butyl ester exhibited the best antimicrobial activity (MIC = 12 μM) and selectivity (TI = 33) among all SLs tested. Kinetic studies revealed that SL-ester derivatives kill B. cereus in a time-dependent manner resulting in greater than a 3-log reduction in cell number within 1 h at 2×MIC. In contrast, lactonic SL required 3 h to achieve the same efficiency. Full article

(This article belongs to the Special Issue Sustainable Chemistry in the Organic Synthesis of Bioactive Compounds)

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Review

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23 pages, 5129 KiB

Open AccessReview

Towards Antibiotic Synthesis in Continuous-Flow Processes

by Marziale Comito, Riccardo Monguzzi, Silvia Tagliapietra, Giovanni Palmisano and Giancarlo Cravotto

Molecules 2023, 28(3), 1421; https://doi.org/10.3390/molecules28031421 - 02 Feb 2023

Cited by 1 | Viewed by 2478

Abstract

Continuous-flow chemistry has become a mainstream process and a notable trend among emerging technologies for drug synthesis. It is routinely used in academic and industrial laboratories to generate a wide variety of molecules and building blocks. The advantages it provides, in terms of safety, speed, cost efficiency and small-equipment footprint compared to analog batch processes, have been known for some time. What has become even more important in recent years is its compliance with the quality objectives that are required by drug-development protocols that integrate inline analysis and purification tools. There can be no doubt that worldwide government agencies have strongly encouraged the study and implementation of this innovative, sustainable and environmentally friendly technology. In this brief review, we list and evaluate the development and applications of continuous-flow processes for antibiotic synthesis. This work spans the period of 2012–2022 and highlights the main cases in which either active ingredients or their intermediates were produced under continuous flow. We hope that this manuscript will provide an overview of the field and a starting point for a deeper understanding of the impact of flow chemistry on the broad panorama of antibiotic synthesis. Full article

(This article belongs to the Special Issue Sustainable Chemistry in the Organic Synthesis of Bioactive Compounds)

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