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Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives
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Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives

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

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 22269

Special Issue Editor

Prof. Dr. Mohamed Abarbri

E-Mail Website
Guest Editor
Laboratoire de Physico-Chimie des Matériaux et des Electrolytes Pour l’Energie (PCM2E), EA 6299, Avenue Monge, Faculté des Sciences, Université de Tours, Parc de Grandmont, 37200 Tours, France
Interests: synthesis of fluorinated compounds; synthesis of heterocyclic compounds; synthesis of compounds of biological interest; organic materials and development of new technologies for energy storage
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

I’m serving as the Guest Editor of a special issue in the journal Molecules (https://www.mdpi.com/journal/molecules). The special issue is focused on “Synthetic Approaches and therapeutic potential of Pyrimidine Derivatives”.
I would like to invite you to contribute a full research article or a comprehensive review in this Special Issue. We think you could make an excellent contribution based on your expertise in this field.

This Special Issue will focus on new advances in the synthesis of this important ring and other Medicinal aspects in an attempt to sheld the light to assist in discovery of novel pyrimidine-based derivatives.

In doing so, we placed specific emphasis on original research papers and short reviews of the synthesis of biologically active pyrimidine compounds using original synthetic approaches.

The deadline for manuscript submission will be 15 September 2021.

For detailed information, please follow the link below to the Special Issue website at: 

Website: https://www.mdpi.com/journal/molecules/special_issues/Pyrimidine

We are looking forward to hearing from you

Prof. Mohamed Abarbri
Guest Editor

Manuscript Submission Information

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Keywords

  • Synthesis
  • Pyrimidine derivatives
  • Biological interest

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Published Papers (7 papers)

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Research

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12 pages, 6758 KiB  
Article
Three Component One-Pot Synthesis and Antiproliferative Activity of New [1,2,4]Triazolo[4,3-a]pyrimidines
by Manel Ben Hassen, Dhouha Msalbi, Badr Jismy, Fares Elghali, Sami Aifa, Hassan Allouchi, Mohamed Abarbri and Fakher Chabchoub
Molecules 2023, 28(9), 3917; https://doi.org/10.3390/molecules28093917 - 5 May 2023
Cited by 7 | Viewed by 1657
Abstract
A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives was prepared using a one-pot three-component synthesis from 5-amino-1-phenyl-1H-1,2,4-triazoles, aromatic aldehydes and ethyl acetoacetate. The compound structures were confirmed by IR, 1H-NMR, 13C-NMR, HRMS and X-ray analyses. The biological activity of these compounds [...] Read more.
A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives was prepared using a one-pot three-component synthesis from 5-amino-1-phenyl-1H-1,2,4-triazoles, aromatic aldehydes and ethyl acetoacetate. The compound structures were confirmed by IR, 1H-NMR, 13C-NMR, HRMS and X-ray analyses. The biological activity of these compounds as antitumor agents was evaluated. Their antitumor activities against cancer cell lines (MDA-MB-231 and MCF-7) were tested by the MTT in vitro method. Among them, compounds 4c and 4j displayed the best antitumor activity with IC50 values of 17.83 μM and 19.73 μM against MDA-MB-231 and MCF-7 cell lines, respectively, compared to the Cisplatin reference. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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17 pages, 5251 KiB  
Article
Synthesis and Molecular Docking Study of Novel Pyrimidine Derivatives against COVID-19
by Zahra M. Alamshany, Reham R. Khattab, Nasser A. Hassan, Ahmed A. El-Sayed, Mohamed A. Tantawy, Ahmed Mostafa and Allam A. Hassan
Molecules 2023, 28(2), 739; https://doi.org/10.3390/molecules28020739 - 11 Jan 2023
Cited by 12 | Viewed by 2111
Abstract
A novel series of pyrido[2,3-d]pyrimidines; pyrido[3,2-e][1,3,4]triazolo; and tetrazolo[1,5-c]pyrimidines were synthesized via different chemical transformations starting from pyrazolo[3,4-b]pyridin-6-yl)-N,N-dimethylcarbamimidic chloride 3b (prepared from the reaction of o-aminonitrile 1b and phosogen iminiumchloride). The [...] Read more.
A novel series of pyrido[2,3-d]pyrimidines; pyrido[3,2-e][1,3,4]triazolo; and tetrazolo[1,5-c]pyrimidines were synthesized via different chemical transformations starting from pyrazolo[3,4-b]pyridin-6-yl)-N,N-dimethylcarbamimidic chloride 3b (prepared from the reaction of o-aminonitrile 1b and phosogen iminiumchloride). The structures of the newly synthesized compounds were elucidated based on spectroscopic data and elemental analyses. Designated compounds are subjected for molecular docking by using Auto Dock Vina software in order to evaluate the antiviral potency for the synthesized compounds against SARS-CoV-2 (2019-nCoV) main protease M pro. The antiviral activity against SARS-CoV-2 showed that tested compounds 7c, 7d, and 7e had the most promising antiviral activity with lower IC50 values compared to Lopinavir, “the commonly used protease inhibitor”. Both in silico and in vitro results are in agreement. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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15 pages, 470 KiB  
Article
Synthesis and Antiprotozoal Activity of Azabicyclo-Nonane Pyrimidine Hybrids
by Clemens Hinteregger, Johanna Dolensky, Werner Seebacher, Robert Saf, Pascal Mäser, Marcel Kaiser and Robert Weis
Molecules 2023, 28(1), 307; https://doi.org/10.3390/molecules28010307 - 30 Dec 2022
Cited by 2 | Viewed by 1390
Abstract
2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes possess activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against pathogens of malaria tropica and sleeping sickness. The activities and selectivities of compounds strongly depended on the substitution pattern of both ring systems [...] Read more.
2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes possess activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against pathogens of malaria tropica and sleeping sickness. The activities and selectivities of compounds strongly depended on the substitution pattern of both ring systems as well as on the position of the nitrogen atom in the bicycles. The most promising hybrids of 3-azabicyclo-nonane with 2-aminopyrimidine showed activity against P. falciparum NF54 in submicromolar concentration and high selectivity. A hybrid with pyrrolidino substitution of the 2-azabicyclo-nonane as well as of the pyrimidine moiety exhibited promising activity against the multiresistant K1 strain of P. falciparum. A couple of hybrids of 2-azabicyclo-nonanes with 2-(dialkylamino)pyrimidines possessed high activity against Trypanosoma brucei rhodesiense STIB900 and good selectivity. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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15 pages, 1807 KiB  
Article
6-(Tetrazol-5-yl)-7-aminoazolo[1,5-a]pyrimidines as Novel Potent CK2 Inhibitors
by Grigoriy V. Urakov, Konstantin V. Savateev, Svetlana K. Kotovskaya, Vladimir L. Rusinov, Alexandr A. Spasov, Denis A. Babkov and Elena V. Sokolova
Molecules 2022, 27(24), 8697; https://doi.org/10.3390/molecules27248697 - 8 Dec 2022
Cited by 1 | Viewed by 1558
Abstract
In this work, we describe the design, synthesis, and structure-activity relationship of 6-(tetrazol-5-yl)-7-aminoazolo[1,5-a]pyrimidines as inhibitors of Casein kinase 2 (CK2). At first, we optimized the reaction conditions for the azide-nitrile cycloaddition in the series of 6-cyano-7-aminoazolopyridimines and sodium azide. The regioselectivity [...] Read more.
In this work, we describe the design, synthesis, and structure-activity relationship of 6-(tetrazol-5-yl)-7-aminoazolo[1,5-a]pyrimidines as inhibitors of Casein kinase 2 (CK2). At first, we optimized the reaction conditions for the azide-nitrile cycloaddition in the series of 6-cyano-7-aminoazolopyridimines and sodium azide. The regioselectivity of this process has been shown, as the cyano group of the pyrimidine cycle was converted to tetrazole while the nitrile of the azole fragment did not react. The desired tetrazolyl-azolopyrimidines were obtained in a moderate to excellent yields (42–95%) and converted further to water soluble sodium salts by the action of sodium bicarbonate. The obtained 6-(tetrazol-5-yl)-7-aminopyrazolo[1,5-a]pyrimidines 2a–k and their sodium salts 3a–c, 3g–k showed nano to low micromolar range of CK2 inhibition while corresponding [1,2,4]triazolopyrimidines 10a–k were less active (IC50 > 10 µM). The leader compound 3-phenyl-6-(tetrazol-5-yl)-7-aminopyrazolo[1,5-a]pyrimidine 2i as CK2 inhibitor showed IC50 45 nM. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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11 pages, 7132 KiB  
Article
Synthesis, Anticancer Activities and Molecular Docking Studies of a Novel Class of 2-Phenyl-5,6,7,8-tetrahydroimidazo [1,2-b]pyridazine Derivatives Bearing Sulfonamides
by Otmane Bourzikat, Abdelmoula El Abbouchi, Hamza Ghammaz, Nabil El Brahmi, Elmostfa El Fahime, Arnaud Paris, Richard Daniellou, Franck Suzenet, Gérald Guillaumet and Saïd El Kazzouli
Molecules 2022, 27(16), 5238; https://doi.org/10.3390/molecules27165238 - 17 Aug 2022
Cited by 10 | Viewed by 2474
Abstract
In the present study, new 2-phenyl-5,6,7,8-tetrahydroimidazo [1,2-b]pyridazines bearing sulfonamides were synthesized, characterized and evaluated for their anticancer activities. The structures of these derivatives were elucidated by 1H NMR, 13C NMR, infrared and high-resolution mass spectrometry for further validation of [...] Read more.
In the present study, new 2-phenyl-5,6,7,8-tetrahydroimidazo [1,2-b]pyridazines bearing sulfonamides were synthesized, characterized and evaluated for their anticancer activities. The structures of these derivatives were elucidated by 1H NMR, 13C NMR, infrared and high-resolution mass spectrometry for further validation of the target compound structures. The anticancer activities of the new molecules were evaluated against five human cancer cell lines, including A-549, Hs-683, MCF-7, SK-MEL-28 and B16-F10 cell lines using 5-fluorouracil and etoposide as the reference drugs. Among the tested compounds, 4e and 4f exhibited excellent activities in the same range of the positive controls, 5-fluorouracil and etoposide, against MCF-7 and SK-MEL-28 cancer cell lines, with IC50 values ranging from 1 to 10 μM. The molecular docking studies of 4e and 4f showed a strong binding with some kinases, which are linked to MCF-7 and SK-MEL-28 cancer cell lines. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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15 pages, 4072 KiB  
Article
A New Class of Uracil–DNA Glycosylase Inhibitors Active against Human and Vaccinia Virus Enzyme
by Inga R. Grin, Grigory V. Mechetin, Rustem D. Kasymov, Evgeniia A. Diatlova, Anna V. Yudkina, Sergei N. Shchelkunov, Irina P. Gileva, Alexandra A. Denisova, Grigoriy A. Stepanov, Ghermes G. Chilov and Dmitry O. Zharkov
Molecules 2021, 26(21), 6668; https://doi.org/10.3390/molecules26216668 - 3 Nov 2021
Cited by 9 | Viewed by 3154
Abstract
Uracil–DNA glycosylases are enzymes that excise uracil bases appearing in DNA as a result of cytosine deamination or accidental dUMP incorporation from the dUTP pool. The activity of Family 1 uracil–DNA glycosylase (UNG) activity limits the efficiency of antimetabolite drugs and is essential [...] Read more.
Uracil–DNA glycosylases are enzymes that excise uracil bases appearing in DNA as a result of cytosine deamination or accidental dUMP incorporation from the dUTP pool. The activity of Family 1 uracil–DNA glycosylase (UNG) activity limits the efficiency of antimetabolite drugs and is essential for virulence in some bacterial and viral infections. Thus, UNG is regarded as a promising target for antitumor, antiviral, antibacterial, and antiprotozoal drugs. Most UNG inhibitors presently developed are based on the uracil base linked to various substituents, yet new pharmacophores are wanted to target a wide range of UNGs. We have conducted virtual screening of a 1,027,767-ligand library and biochemically screened the best hits for the inhibitory activity against human and vaccinia virus UNG enzymes. Although even the best inhibitors had IC50 ≥ 100 μM, they were highly enriched in a common fragment, tetrahydro-2,4,6-trioxopyrimidinylidene (PyO3). In silico, PyO3 preferably docked into the enzyme’s active site, and in kinetic experiments, the inhibition was better consistent with the competitive mechanism. The toxicity of two best inhibitors for human cells was independent of the presence of methotrexate, which is consistent with the hypothesis that dUMP in genomic DNA is less toxic for the cell than strand breaks arising from the massive removal of uracil. We conclude that PyO3 may be a novel pharmacophore with the potential for development into UNG-targeting agents. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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Review

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34 pages, 116088 KiB  
Review
Biginelli Reaction Mediated Synthesis of Antimicrobial Pyrimidine Derivatives and Their Therapeutic Properties
by Maria Marinescu
Molecules 2021, 26(19), 6022; https://doi.org/10.3390/molecules26196022 - 4 Oct 2021
Cited by 38 | Viewed by 8808
Abstract
Antimicrobial resistance was one of the top priorities for global public health before the start of the 2019 coronavirus pandemic (COVID-19). Moreover, in this changing medical landscape due to COVID-19, finding new organic structures with antimicrobial and antiviral properties is a priority in [...] Read more.
Antimicrobial resistance was one of the top priorities for global public health before the start of the 2019 coronavirus pandemic (COVID-19). Moreover, in this changing medical landscape due to COVID-19, finding new organic structures with antimicrobial and antiviral properties is a priority in current research. The Biginelli synthesis that mediates the production of pyrimidine compounds has been intensively studied in recent decades, especially due to the therapeutic properties of the resulting compounds, such as calcium channel blockers, anticancer, antiviral, antimicrobial, anti-inflammatory or antioxidant compounds. In this review we aim to review the Biginelli syntheses reported recently in the literature that mediates the synthesis of antimicrobial compounds, the spectrum of their medicinal properties, and the structure–activity relationship in the studied compounds. Full article
(This article belongs to the Special Issue Synthetic Approaches and Therapeutic Potential of Pyrimidine Derivatives)
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