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Molecules
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Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds
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Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds

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

Deadline for manuscript submissions: closed (31 May 2022) | Viewed by 10705

Special Issue Editors

Prof. Dr. Sobhi M. Gomha

E-Mail Website
Guest Editor
Chemistry Department, Faculty of Science, Islamic University of Madinah, Al-Madinah Al-Munawwarah, 42351 Saudi Arabia
Interests: green synthesis; heterocyclic compounds; green chemistry; microwave irradiation; ultrasonic radiation; grinding; ionic liquids
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Maher Fathalla

E-Mail Website
Guest Editor
Chemistry Department, Faculty of Science, Islamic University of Madinah, Al-Madinah Al-Munawwarah 42351, Saudi Arabia
Interests: synthetic organic chemistry; porphyrin-based functional nanomaterials; drug delivery; self-assembly and molecular recognition; metal-nanoparticles; bioactive heterocyclic compounds

Special Issue Information

Dear Colleagues,

Heterocyclic compounds are cyclic organic compounds that contain at least one carbon atom and at least one other element such as nitrogen, oxygen, or sulfur. Heterocyclic compounds are essential to life as they are widely distributed in nature. The synthesis and characterizations of bioactive heterocyclic compounds plays a central role in drug discovery arena and has been one of the most active research areas for decades. This special issue of the open access journal, Molecules, devoted to Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds.

Researchers are cordially invited to contribute original research papers or reviews to this special issue of Molecules.

Prof. Dr. Sobhi M. Gomha
Prof. Dr. Maher Fathalla
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

  • organic synthesis
  • heterocycles
  • chemical characterization
  • sustainable synthesis
  • bioactive compounds
  • methodology
  • biological activity
  • reaction mechanism

Published Papers (4 papers)

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Research

19 pages, 9624 KiB  
Article
Synthesis, Molecular Docking Study, and Cytotoxic Activity against MCF Cells of New Thiazole–Thiophene Scaffolds
by Sobhi M. Gomha, Sayed M. Riyadh, Bader Huwaimel, Mohie E. M. Zayed and Magda H. Abdellattif
Molecules 2022, 27(14), 4639; https://doi.org/10.3390/molecules27144639 - 20 Jul 2022
Cited by 18 | Viewed by 1957
Abstract
Investigating novel compounds that may be useful in designing new, less toxic, selective, and potent breast anticancer agents is still the main challenge for medicinal chemists. Thus, in the present work, acetylthiophene was used as a building block to synthesize a novel series [...] Read more.
Investigating novel compounds that may be useful in designing new, less toxic, selective, and potent breast anticancer agents is still the main challenge for medicinal chemists. Thus, in the present work, acetylthiophene was used as a building block to synthesize a novel series of thiazole-bearing thiophene derivatives. The structures of the synthesized compounds were elucidated based on elemental analysis and spectral measurements. The cytotoxic activities of the synthesized compounds were evaluated against MCF-7 tumor cells and compared to a cisplatin reference drug, and against the LLC-Mk2 normal cell line using the MTT assay, and the results revealed promising activities for compounds 4b and 13a. The active compounds were subjected to molecular modeling using MOE 2019, the pharmacokinetics were studied using SwissADME, and a toxicity radar was obtained from the biological screening data. The results obtained from the computational studies supported the results obtained from the anticancer biological studies. Full article
(This article belongs to the Special Issue Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds)
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25 pages, 3074 KiB  
Article
Exploring the Synthetic Potential of γ-Lactam Derivatives Obtained from a Multicomponent Reaction—Applications as Antiproliferative Agents
by Adrián López-Francés, Xabier del Corte, Zuriñe Serna-Burgos, Edorta Martínez de Marigorta, Francisco Palacios and Javier Vicario
Molecules 2022, 27(11), 3624; https://doi.org/10.3390/molecules27113624 - 5 Jun 2022
Cited by 5 | Viewed by 2243
Abstract
A study on the reactivity of 3-amino α,β-unsaturated γ-lactam derivatives obtained from a multicomponent reaction is presented. Key features of the substrates are the presence of an endocyclic α,β-unsaturated amide moiety and an enamine functionality. Following different synthetic protocols, the functionalization at three [...] Read more.
A study on the reactivity of 3-amino α,β-unsaturated γ-lactam derivatives obtained from a multicomponent reaction is presented. Key features of the substrates are the presence of an endocyclic α,β-unsaturated amide moiety and an enamine functionality. Following different synthetic protocols, the functionalization at three different positions of the lactam core is achieved. In the presence of a soft base, under thermodynamic conditions, the functionalization at C-4 takes place where the substrates behave as enamines, while the use of a strong base, under kinetic conditions, leads to the formation of C-5-functionalized γ-lactams, in the presence of ethyl glyoxalate, through a highly diastereoselective vinylogous aldol reaction. Moreover, the nucleophilic addition of organometallic species allows the functionalization at C-3, through the imine tautomer, affording γ-lactams bearing tetrasubstituted stereocenters, where the substrates act as imine electrophiles. Taking into account the advantage of the presence of a chiral stereocenter in C-5 substituted γ-lactams, further diastereoselective transformations are also explored, leading to novel bicyclic substrates holding a fused γ and δ-lactam skeleton. Remarkably, an example of a highly stereoselective formal [3+3] cycloaddition reaction of chiral γ-lactam substrates is reported for the synthesis of 1,4-dihidropyridines, where a non-covalent attractive interaction of a carbonyl group with an electron-deficient arene seems to drive the stereoselectivity of the reaction to the exclusive formation of the cis isomer. In order to unambiguously determine the substitution pattern resulting from the diverse reactions, an extensive characterization of the substrates is detailed through 2D NMR and/or X-ray experiments. Likewise, applications of the substrates as antiproliferative agents against lung and ovarian cancer cells are also described. Full article
(This article belongs to the Special Issue Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds)
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19 pages, 17394 KiB  
Article
Design, Synthesis, Molecular Docking, and Evaluation Antioxidant and Antimicrobial Activities for Novel 3-Phenylimidazolidin-4-One and 2-Aminothiazol-4-One Derivatives
by Wesam S. Shehab, Maged A. Aziz, Nourhan Kh. R. Elhoseni, Mohamed G. Assy, Magda H. Abdellattif and Eman O. Hamed
Molecules 2022, 27(3), 767; https://doi.org/10.3390/molecules27030767 - 25 Jan 2022
Cited by 8 | Viewed by 2623
Abstract
On our way to discovering and developing compounds that have an antioxidant impact compared to ascorbic acid and other biological activities, we designed, synthesized, and evaluated a new series of heterocyclic moieties drugs (1–11) as antioxidants and antimicrobial agents. [...] Read more.
On our way to discovering and developing compounds that have an antioxidant impact compared to ascorbic acid and other biological activities, we designed, synthesized, and evaluated a new series of heterocyclic moieties drugs (1–11) as antioxidants and antimicrobial agents. As starting moieties, these new candidates were derived from two promising heterocyclic compounds, imidazoldin-4-one and thiazol-4-one. Firstly, diphenylimidazol 1 was obtained because of the cyclo condensation one-pot ternary reaction of urea, aniline, and chloroacetic acid under thermal conditions. Out of this starting compound, we could design and create new vital rings such as purine and triazine as in compounds 5 and 6, respectively. Secondly, the start thiazole derivative 7 was obtained from the intermolecular cyclization of thiourea, chloroacetic acid, p-nitobezaldehyde in the presence of sodium acetate. We synthesized various derivatives from this second starting compound 7 by being subjected to different reagents such as aniline, phenylenediamine, phenylhydrazine, and barbituric acid to yield 8, 9, 10, and 11, respectively. Using ascorbic acid as the standard compound, the pharmacological testing for antioxidant activity assessment of the produced derivatives was evaluated against ABTS (2,20-azinobis (3-ethylbenzothiazoline-6-sulfonic acid). Candidate 6 exhibited the best activity as an antioxidant agent compared to ascorbic acid as a reference compound. Moreover, all compounds were evaluated as antimicrobial agents against a series of bacteria and fungi. Among all synthesized compounds, compound 6 achieved high efficiency against two types of fungi and four kinds of bacteria, as Clotrimazole and Ampicillin were used as the reference agents, respectively. All chemical structures of the novel synthesized candidates were unequivocally elucidated and confirmed utilizing spectroscopical and elemental investigations. Full article
(This article belongs to the Special Issue Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds)
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22 pages, 2588 KiB  
Article
Investigation of the Anticancer Effect of α-Aminophosphonates and Arylidine Derivatives of 3-Acetyl-1-aminoquinolin-2(1H)-one on the DMBA Model of Breast Cancer in Albino Rats with In Silico Prediction of Their Thymidylate Synthase Inhibitory Effect
by Mohamed A. Nassan, Adil Aldhahrani, Hamada H. Amer, Ahmed Elhenawy, Ayman A. Swelum, Omar M. Ali and Yasser H. Zaki
Molecules 2022, 27(3), 756; https://doi.org/10.3390/molecules27030756 - 24 Jan 2022
Cited by 11 | Viewed by 2954
Abstract
Breast cancer is a major cause of death in women worldwide. In this study, 60 female rats were classified into 6 groups; negative control, α-aminophosphonates, arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one, DMBA, DMBA & α-aminophosphonates, and DMBA & arylidine derivatives of [...] Read more.
Breast cancer is a major cause of death in women worldwide. In this study, 60 female rats were classified into 6 groups; negative control, α-aminophosphonates, arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one, DMBA, DMBA & α-aminophosphonates, and DMBA & arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one. New α-aminophosphonates and arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one were synthesized and elucidated by different spectroscopic and elemental analysis. Histopathological examination showed marked proliferation of cancer cells in the DMBA group. Treatment with α-aminophosphonates mainly decreased tumor mass. Bcl2 expression increased in DMBA-administered rats and then declined in the treated groups, mostly with α-aminophosphonates. The level of CA15-3 markedly declined in DMBA groups treated with α-aminophosphonates and arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one. Gene expression of GST-P, PCNA, PDK, and PIK3CA decreased in the DMBA group treated with α-aminophosphonates and arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one, whereas PIK3R1 and BAX increased in the DMBA group treated with α-aminophosphonates and arylidine derivatives of 3-acetyl-1-aminoquinolin-2(1H)-one. The molecular docking postulated that the investigated compounds can inhibt the Thymidylate synthase TM due to high hydrophobicity charachter. Full article
(This article belongs to the Special Issue Synthesis, Characterizations and Applications of Bioactive Heterocyclic Compounds)
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