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Synthesis, Application and Biological Evaluation of Chemical Organic Compounds

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A special issue of Processes (ISSN 2227-9717). This special issue belongs to the section "Chemical Processes and Systems".

Deadline for manuscript submissions: closed (25 August 2023) | Viewed by 25997

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Prof. Dr. Iliyan Ivanov

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Guest Editor

Department of Organic Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria
Interests: organic chemistry; synthesis; heterocycles
Special Issues, Collections and Topics in MDPI journals

Dr. Stanimir Manolov

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Guest Editor

Department of Organic Chemistry, University of Plovdiv, 4000 Plovdiv, Bulgaria
Interests: green synthesis; heterogeneous cyclisation; isoquinolines; profens
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The process of the transformation of one molecule into another molecule, which involves building new chemical bonds and breaking existing ones, is of great importance in organic synthesis. The main task of organic synthesis is the obtainment of a variety of organic compounds—both isolated in minimal quantities from natural products and unknown organic molecules, or compounds with certain biological, or other predetermined properties, based on suitable starting materials using various synthetic processes. In essence, organic synthesis is a complex methodology for building organic molecules from individual starting materials, fragments, or synthons. This task is performed by appropriately selected organic reactions, which lead to the production of certain reaction products and ultimately to the target molecules.

Recently, during and before the pandemic of novel SARS-CoV-2, a large number of new organic hybrid molecules were developed using known and newly invented synthetic methodologies, some of which showed outstanding results in the treatment against COVID-19.

With this Special Issue on “Synthesis, Application and Biological Evaluation of Chemical Organic Compounds”, we aim to attract original research articles and review papers that cover research on the synthesis of new organic molecules using newly developed or known synthetic procedures, the evaluation of their biological evaluation, and their application.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

The development of new procedures for the obtainment of organic compounds;
The synthesis of new organic molecules;
The synthesis of hybrid molecules;
The synthesis and biological evaluation of new molecules;
In silico, in vitro, and in vivo biological evaluation of new and/or known organic compounds.

We look forward to receiving your contributions.

Prof. Dr. Iliyan Ivanov
Dr. Stanimir Manolov
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. Processes 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 2400 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.

Published Papers (11 papers)

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Editorial

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4 pages, 200 KiB

Open AccessEditorial

Special Issue: Synthesis, Application, and Biological Evaluation of Chemical Organic Compounds

by Stanimir Manolov and Iliyan Ivanov

Processes 2023, 11(9), 2802; https://doi.org/10.3390/pr11092802 - 21 Sep 2023

Viewed by 590

Abstract

This Special Issue of Processes, entitled “Synthesis, Application, and Biological Evaluation of Chemical Organic Compounds”, gathers the most recent work of leading researchers in a single forum [...] Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

Research

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18 pages, 3399 KiB

Open AccessArticle

Synthesis, Molecular Docking, Molecular Dynamics Studies, and In Vitro Biological Evaluation of New Biofunctional Ketoprofen Derivatives with Different N-Containing Heterocycles

by Stanimir Manolov, Dimitar Bojilov, Iliyan Ivanov, Gabriel Marc, Nadezhda Bataklieva, Smaranda Oniga, Ovidiu Oniga and Paraskev Nedialkov

Processes 2023, 11(6), 1837; https://doi.org/10.3390/pr11061837 - 17 Jun 2023

Cited by 2 | Viewed by 1411

Abstract

Herein, we report the synthesis of four new hybrid molecules between ketoprofen or 2-(3-benzoylphenyl)propanoic acid and N-containing heterocyclic compounds, such as piperidine, pyrrolidine, 1,2,3,4-tetrahydroquinoline, and 1,2,3,4-tetrahydroisoquinoline. The obtained hybrid compounds were fully characterized using ¹H- and ¹³C-NMR, UV-Vis, and HRMS spectra. Detailed HRMS analysis is provided for all novel hybrid molecules. The compounds were assessed for their in vitro anti-inflammatory and antioxidant activity. The lipophilicity of the hybrids was determined, both theoretically (cLogP) and experimentally (R_M). The affinity of the compounds to the human serum albumin was assessed in silico by molecular docking study using two software, and the stability of the predicted complexes was evaluated by molecular dynamics study. All novel hybrids have shown very good HPSA activity, statistically close when compared to the reference—quercetin. The molecular docking confirmed the obtained in vitro results. Tetrahydroquinoline derivative 3c and tetrahydroisoquinoline derivative 3d have the highest affinity for albumin. They show stronger anti-inflammatory action than their predecessor, ketoprofen and the regularly used ibuprofen. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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21 pages, 2039 KiB

Open AccessArticle

Sustainable Bioactive Composite of Glehnia littoralis Extracts for Osteoblast Differentiation and Bone Formation

by Chul Joong Kim, Bimal Kumar Ghimire, Seon Kang Choi, Chang Yeon Yu and Jae Geun Lee

Processes 2023, 11(5), 1491; https://doi.org/10.3390/pr11051491 - 15 May 2023

Cited by 3 | Viewed by 1552

Abstract

Different bone-related diseases are mostly caused by the disruption of bone formation and bone resorption, including osteoporosis. Traditional medicinal literature has reported the possible anti-osteoporotic properties of Glehnia littoralis. However, the chemical compounds in extracts that are responsible for bone metabolism are poorly understood. The present study aimed to explore and compare the coumarin-based compounds present in G. littoralis extracts, the antioxidant activities, and the anti-osteoporotic properties of different extracts of G. littoralis (leaf and stem, fruit, whole plant, and root extracts) on bone metabolism. This study analyzed G. littoralis extract effects on the proliferation and osteoblastic differentiation of MC3T3-E1 osteoblasts. Among the different tested samples, stem extracts had the highest scopoletin (53.0 mg/g), and umbelliferone (1.60 mg/g). The significantly (p < 0.05) highest amounts of imperatorin (31.9 mg/g) and phellopterin (2.3 mg/g), were observed in fruit and whole plant extracts, respectively. Furthermore, the results confirmed alkaline phosphatase activity, collagen synthesis, mineralization, osteocalcin content, and osterix and RUNX2 expression. G. littoralis extracts at concentrations greater than 20 µg/mL had particularly adverse effects on MC3T3-E1 cell viability and proliferation. Notably, cell proliferation was significantly elevated at lower G. littoralis concentrations. Comparatively, 0.5 µg/mL stem had a higher osteocalcin content. Of the four extract types, stem showed a higher collagen synthesis effect at concentrations of 0.5–5 µg/mL. Except for fruit extracts, G. littoralis extract treatment significantly elevated osterix gene expression. All G. littoralis extracts increased RUNX2 gene expression. The results described here indicate that G. littoralis ethanolic extracts can effectively prevent osteoporosis. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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13 pages, 3802 KiB

Open AccessArticle

Novel Non-Toxic Highly Antibacterial Chitosan/Fe(III)-Based Nanoparticles That Contain a Deferoxamine—Trojan Horse Ligands: Combined Synthetic and Biological Studies

by Omar M. Khubiev, Victoria E. Esakova, Anton R. Egorov, Artsiom E. Bely, Roman A. Golubev, Maxim V. Tachaev, Anatoly A. Kirichuk, Nikolai N. Lobanov, Alexander G. Tskhovrebov and Andreii S. Kritchenkov

Processes 2023, 11(3), 870; https://doi.org/10.3390/pr11030870 - 14 Mar 2023

Cited by 5 | Viewed by 1420

Abstract

In this study, we prepared chitosan/Fe(III)/deferoxamine nanoparticles with unimodal size distribution (hydrodynamic diameter ca. 250 nm, zeta potential ca. 32 mV). The elaborated nanoparticles are characterized by outstanding in vitro and in vivo antibacterial activity, which exceeds even that of commercial antibiotics ampicillin and gentamicin. Moreover, the nanoparticles are non-toxic. We found that the introduction of iron ions into the chitosan matrix increases the ability of the resulting nanoparticles to disrupt the integrity of the membranes of microorganisms in comparison with pure chitosan. The introduction of deferoxamine into the obtained nanoparticles sharply expands their effect of destruction the bacterial membrane. The obtained antibacterial nanoparticles are promising for further preclinical studies. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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19 pages, 5732 KiB

Open AccessArticle

Procainamide Charge Transfer Complexes with Chloranilic Acid and 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone: Experimental and Theoretical Study

by A. F. M. Motiur Rahman, Ahmed H. Bakheit, Shofiur Rahman, Gamal A. E. Mostafa and Haitham Alrabiah

Processes 2023, 11(3), 711; https://doi.org/10.3390/pr11030711 - 27 Feb 2023

Cited by 2 | Viewed by 1174

Abstract

The formation of charge transfer (CT) complexes between bioactive molecules and/or organic molecules is an important aspect in order to understand ‘molecule-receptor’ interactions. Here, we have synthesized two new CT complexes, procainamide-chloranilic acid (PA-ChA) and procainamide-2,3-dichloro-5,6-dicyano-1,4-benzoquinone (PA-DDQ), from electron donor procainamide (PA), electron acceptor chloranilic acid (ChA), and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). The structures of these two CT complexes were elucidated/characterized using FTIR, NMR, and many other spectroscopic methods. A stability study of each complex was conducted for the first time using various spectroscopic parameters (e.g., formation constant, molar extinction coefficient, ionization potential oscillator strength, dipole moment, and standard free energy). The formation of CT complexes in solution was confirmed by spectrophotometric determination. The molecular composition of each complex was determined using the spectrophotometric titration method and gave a 1:1 (donor:acceptor) ratio. In addition, the formation constant was determined using the Benesi–Hildebrand equation. To understand the noncovalent interactions of the complexes, density functional theory (DFT) calculations were performed using the ωB97XD/6-311++G(2d,p) level of theory. The DFT-computed interaction energies (ΔIEs) and the Gibbs free energies (ΔGs) were in the same order as observed experimentally. The DFT-calculated results strongly support our experimental results. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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11 pages, 2293 KiB

Open AccessFeature PaperArticle

Evaluation of Antiaging Effect of Sheep Placenta Extract Using SAMP8 Mice

by Ming-Yu Chou, Chi-Pei Ou Yang, Wen-Ching Li, Yao-Ming Yang, Yu-Ju Huang, Ming-Fu Wang and Wan-Teng Lin

Processes 2022, 10(11), 2242; https://doi.org/10.3390/pr10112242 - 01 Nov 2022

Cited by 5 | Viewed by 9344

Abstract

Widely used in traditional medicine, sheep placenta extract (SPE) is known for its physiological effects such as wound healing, antioxidant, and anti-inflammatory properties. However, the effect of SPE on antiaging is still unclear. In this study, we investigated the effect of SPE on aging through the senescence-accelerated mouse prone 8 (SAMP8) strain. We designed an experiment using both male and female mice randomly divided into 4 groups (n = 10) as follows: Group A—control group; Group B—low-dose SPE (61.5 mg/kg BW/day); Group C—medium-dose SPE (123 mg/kg BW/day); and Group D—high-dose SPE (184.5 mg/kg BW/day). As a result of measuring the aging index parameters such as skin glossiness, spine lordosis, and kyphosis, it was found that the treatment of SPE lowered the aging index. In addition, we found that biochemical parameters such as lactic acid, glucose, ketone bodies, free fatty acids, tumor necrosis factor-alpha (TNF-α), and interleukin 6 (IL-6) were not changed in the experimental group treated with SPE for 13 weeks. Finally, we found that lipid peroxidation (LPO) was decreased, while the activities of catalase and superoxide dismutase (SOD) were significantly increased in the brain tissues of SPE-treated male and female mice. Supplementation of SPE lowered the oxidative stress caused by the aging process in mice without toxicity and decreased the aging index, suggesting the value of SPE as an effective antiaging treatment. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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13 pages, 2128 KiB

Open AccessArticle

Synthesis, In Silico, and In Vitro Biological Evaluation of New Furan Hybrid Molecules

by Stanimir Manolov, Iliyan Ivanov, Dimitar Bojilov and Paraskev Nedialkov

Processes 2022, 10(10), 1997; https://doi.org/10.3390/pr10101997 - 02 Oct 2022

Cited by 4 | Viewed by 1309

Abstract

Herein, we report the synthesis of new hybrid molecules between furan and N-containing heterocyclic compounds such as pyrrolidine, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroisoquinoline, and piperidine. The obtained compounds were fully characterized using ¹H- and ¹³C-NMR, UV-Vis, and HRMS spectra. All compounds were assessed for their anti-inflammatory, anti-arthritic, antioxidant, reducing power ability, and chelating activity. The less lipophilic molecules H2 (60.1 ± 8.16) and H4 (62.23 ± 0.83) had almost 12 times higher ATA compared with the used ketoprofen (720.57 ± 19.78) standard. The inhibition of albumin denaturation results makes the newly obtained hybrids potential anti-inflammatory drugs, as the expressed values are higher than the ketoprofen standard (126.58 ± 5.00), except H3 (150.99 ± 1.16). All four compounds show significant activity regarding the in vitro biological activities, which makes them great candidates for potential future drugs. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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13 pages, 2012 KiB

Open AccessArticle

Synthesis, Characterization, and Antibacterial Potential of Poly(o-anisidine)/BaSO₄ Nanocomposites with Enhanced Electrical Conductivity

by Mirza Nadeem Ahmad, Sohail Nadeem, Raya Soltane, Mohsin Javed, Shahid Iqbal, Zunaira Kanwal, Muhammad Fayyaz Farid, Sameh Rabea, Eslam B. Elkaeed, Samar O. Aljazzar, Hamad Alrbyawi and Walid F. Elkhatib

Processes 2022, 10(9), 1878; https://doi.org/10.3390/pr10091878 - 16 Sep 2022

Cited by 8 | Viewed by 1682

Abstract

The poly(o-anisidine)/BaSO₄ nanocomposites were prepared by oxidative polymerization of o-anisidine monomer with BaSO₄ filler for the potential antibacterial properties of the composite materials. To achieve the optimal and tunable properties of the nanocomposites, the ratio of BaSO₄ filler was changed at the rates of 1%, 3%, 5%, 7%, and 10% with respect to matrix. Different analytical techniques, i.e., FTIR and UV-visible spectroscopy, were employed for functional identification and optical absorption of the poly(o-anisidine)/BaSO₄ nanocomposites. The FTIR data revealed the significant interaction between POA and BaSO₄, as well as the good absorption behavior of the UV-visible spectra. The conducting properties were controllable by varying the load percentage of the BaSO₄ filler. Furthermore, different bacterial strains, i.e., Pseudomonas aeruginosa (Gram-negative) and Staphylococcus aureus (Gram-positive), were used to evaluate the antibacterial activity of the POA/BaSO₄ nanocomposites. The largest zones of inhibition 0.8 and 0.9 mm were reached using 7% and 10% for Staphylococcus aureus and Pseudomonas aeruginosa, respectively. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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27 pages, 1899 KiB

Open AccessArticle

Synthesis, Characterization, and Biological Evaluation of Novel N-{4-[(4-Bromophenyl)sulfonyl]benzoyl}-L-valine Derivatives

by Theodora-Venera Apostol, Mariana Carmen Chifiriuc, Laura-Ileana Socea, Constantin Draghici, Octavian Tudorel Olaru, George Mihai Nitulescu, Diana-Carolina Visan, Luminita Gabriela Marutescu, Elena Mihaela Pahontu, Gabriel Saramet and Stefania-Felicia Barbuceanu

Processes 2022, 10(9), 1800; https://doi.org/10.3390/pr10091800 - 07 Sep 2022

Cited by 1 | Viewed by 2118

Abstract

In this article, we present the design and synthesis of novel compounds, containing in their molecules an L-valine residue and a 4-[(4-bromophenyl)sulfonyl]phenyl moiety, which belong to N-acyl-α-amino acids, 4H-1,3-oxazol-5-ones, 2-acylamino ketones, and 1,3-oxazoles chemotypes. The synthesized compounds were characterized through elemental analysis, MS, NMR, UV/VIS, and FTIR spectroscopic techniques, the data obtained being in accordance with the assigned structures. Their purities were verified by reversed-phase HPLC. The new compounds were tested for antimicrobial action against bacterial and fungal strains, for antioxidant activity by DPPH, ABTS, and ferric reducing power assays, and for toxicity on freshwater cladoceran Daphnia magna Straus. Furthermore, in silico studies were performed concerning the potential antimicrobial effect and toxicity. The results of antimicrobial activity, antioxidant effect, and toxicity assays, as well as of in silico analysis revealed a promising potential of N-{4-[(4-bromophenyl)sulfonyl]benzoyl}-L-valine and 2-{4-[(4-bromophenyl)sulfonyl]phenyl}-4-isopropyl-4H-1,3-oxazol-5-one for developing novel antimicrobial agents to fight Gram-positive pathogens, and particularly Enterococcus faecium biofilm-associated infections. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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25 pages, 12323 KiB

Open AccessArticle

The Assessment of Anticancer and VEGFR-2 Inhibitory Activities of a New 1H-Indole Derivative: In Silico and In Vitro Approaches

by Eslam B. Elkaeed, Reda G. Yousef, Hazem Elkady, Ibraheem M. M. Gobaara, Aisha A. Alsfouk, Dalal Z. Husein, Ibrahim M. Ibrahim, Ahmed M. Metwaly and Ibrahim H. Eissa

Processes 2022, 10(7), 1391; https://doi.org/10.3390/pr10071391 - 17 Jul 2022

Cited by 36 | Viewed by 2543

Abstract

Corresponding to the reported features of anti-VEGFR-2-approved compounds, a new 1H-indole derivative (compound 7) was designed. The inhibitory potential of the designed compound was revealed via a molecular docking study that showed the appropriate binding. Then, MD simulation (six studies) over a period of 100 ns was performed to confirm the precise binding and optimum energy. Additionally, MM-GBSA reaffirmed the perfect binding, exhibiting a total precise energy of −40.38 Kcal/Mol. The MM-GBSA experiments named the essential amino acids in the protein–ligand interaction, employing the binding energy decomposition and revealing the diversity of interactions of compound 7 inside the VEGFR-2 enzyme. As compound 7 is new, DFT experiments were utilized for molecular structure optimization. Additionally, the DFT results validated the coherent interaction of compound 7 with the VEGFR-2 enzyme. A good value of drug-likeness of compound 7 was acknowledged via in silico ADMET studies. Interestingly, the experimental in vitro prohibitory potential of compound 7 was better than that of sorafenib, demonstrating an IC₅₀ value of 25 nM. Notably, the strong inhibitory effects of compound 10 against two cancer cell lines (MCF-7 and HCT 116) were established with IC₅₀ values of 12.93 and 11.52 μM, disclosing high selectivity indexes of 6.7 and 7.5, respectively. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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Other

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7 pages, 934 KiB

Open AccessOpinion

Hydrogen/Deuterium Exchange in Ambrox Could Improve the Long-Term Scent and Shelf Life of Perfumes

by Antonio Rosales Martínez and Ignacio Rodríguez-García

Processes 2023, 11(8), 2358; https://doi.org/10.3390/pr11082358 - 05 Aug 2023

Cited by 1 | Viewed by 1126

Abstract

Ambrox is a marine natural compound with a delicious ambergris-type scent widely used in fine perfumery. The increase in the long-term scent and shelf life of perfumes has become a paramount endeavor in the fragrance industry. To the best of our knowledge, the exchange of hydrogen by deuterium to decrease the volatility of the constituents of a perfume has not yet been investigated. In this article, we propose this new use of deuteration to synthesize deuterated ambrox in order to decrease its volatility and improve the long-term scent and extend the shelf-life of perfumes. Full article

(This article belongs to the Special Issue Synthesis, Application and Biological Evaluation of Chemical Organic Compounds)

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