Recent synthetic methodologies for pyrimidine and its derivatives

Ibraheem, Farhat; Saddique, Furqan Ahmad; Aslam, Sana; Mansha, Asim; Farooq, Tahir; Ahmad, Matloob

doi:10.3906/kim-1806-8

Cited by 5 publications

(3 citation statements)

References 48 publications

(53 reference statements)

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“…In recent years, a large number of studies has been done on the synthesis and evaluation of the antibacterial properties of pyrimidine derivatives [224][225][226][227][228][229][230][231] and in this context significant attention has been paid to the identification, synthesis, and evaluation of the antibacterial properties of pyrimidine/imidazole hybrids with potentially significant activity [232][233][234][235].…”

Section: Pyrimidine/imidazole Hybridsmentioning

confidence: 99%

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

Rossi

Ciofalo

2020

Molecules

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The rapid growth of serious infections caused by antibiotic resistant bacteria, especially the nosocomial ESKAPE pathogens, has been acknowledged by Governments and scientists and is one of the world’s major health problems. Various strategies have been and are currently investigated and developed to reduce and/or delay the bacterial resistance. One of these strategies regards the design and development of antimicrobial hybrids and conjugates. This unprecedented critical review, in which our continuing interest in the synthesis and evaluation of the bioactivity of imidazole derivatives is testified, aims to summarise and comment on the results obtained from the end of the 1900s until February 2020 in studies conducted by numerous international research groups on the synthesis and evaluation of the antibacterial properties of imidazole-based molecular hybrids and conjugates in which the pharmacophoric constituents of these compounds are directly covalently linked or connected through a linker or spacer. In this review, significant attention was paid to summarise the strategies used to overcome the antibiotic resistance of pathogens whose infections are difficult to treat with conventional antibiotics. However, it does not include literature data on the synthesis and evaluation of the bioactivity of hybrids and conjugates in which an imidazole moiety is fused with a carbo- or heterocyclic subunit.

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Section: Pyrimidine/imidazole Hybridsmentioning

confidence: 99%

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

Rossi

Ciofalo

2020

Molecules

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“…Pyrimidines and their oxo-derivatives are well researched due to important biological evaluation of molecules that contain these nuclei [1][2][3][4]. Recent reports indicate that these compounds are associated with many pharmacological roles such as antiinflammation [5], antitubercular [6], anticancer [7], antimicrobial [8], analgesic [9], antinociceptive [10], antiplasmodial [11], anti-hepatitis C viral, anti-HIV-1 integrase, and calcium channel blocker [12].…”

Section: Introductionmentioning

confidence: 99%

One‐pot three‐component reaction; synthesis of new symmetrically bridge 4,4′‐(1,4‐phenylene)di‐pyrimidines under solvent free conditions

Mohamed

Abdelmeged

Shaker

et al. 2021

Journal of Heterocyclic Chem

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The present article describes a facile one-pot synthesis of a new series of 4,4 0 -(1,4-phenylene)-dipyrimidines (6a-c and 10a, b) by the reaction of terephthalaldehyde (1), 2-acetylthiophene, and/or nitriles with Sbenzylthiouronium chloride 3a. And also, the di-pyrimidinones 13a-d were obtained by the reaction of different amidines 3a-d and ethyl cyanoacetate (11) with terephthalaldehyde (1) under solvent-free conditions in the existence of sodium hydroxide which is found to be a more efficient base for these reactions. The final products were characterized by spectral data and elemental analysis, IR, MS, 1 H, and 13 C NMR spectroscopy.

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“…20 Many efficient synthetic approaches for synthesizing compounds containing pyrimidine ring or its derivatives have been developed and reported. 21,22 However, the reaction of α, β-unsaturated ketones (Chalcones) with urea under acidic or basic conditions is an excellent illustrative method to produce the corresponding 2-pyrimidinone ring. 23,24 Pyrimidine motif and its derivatives are privileged fragments in drug discovery with a wide range of medical applications for example; antioxidant 25 anticancer, 26 antiviral, 27 and antiinflammatory.…”

mentioning

confidence: 99%

Synthesis and Molecular Docking Studies of New Pyrimidinone ring Containing 1,2,3-Triazole Derivatives

Kozan,

Nahi

2023

IJDDT

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The current work describes the design, synthesis and molecular mocking studies of a series of new 1,4-disubstituted-1,2,3-triazole linked 2-pyrimidinone derivatives. Firstly, 4-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)benzene sulfonic acid 1 was synthesized as a key starting material. This compound was reacted with a series of aromatic aldehydes under-investigated conditions to give a new series of chalcones 2a-f. Reaction of compounds 2a-f with urea in the presence of an aqueous solution of sodium hydroxide led to the construct 2-pyrimidinone ring system to obtain a series of new compounds containing 1,2,3-triaozle ring and pyrimidinone ring 3a-f. The newly synthesized compounds 2a-f and 3a-f were characterized by FT-IR, 1H-NMR and 13C-NMR spectra. In-silico molecular docking simulations, compounds 3a-f and their precursors 2a-f were conducted on two selected proteins: 7dpp and 8cx9. The results revealed that all of the newly synthesized compounds 2a-f and 3a-f displayed have a good binding affinity with the target proteins and higher than values recorded for the selected three standard antiviral drugs.

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Recent synthetic methodologies for pyrimidine and its derivatives

Cited by 5 publications

References 48 publications

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

One‐pot three‐component reaction; synthesis of new symmetrically bridge 4,4′‐(1,4‐phenylene)di‐pyrimidines under solvent free conditions

Synthesis and Molecular Docking Studies of New Pyrimidinone ring Containing 1,2,3-Triazole Derivatives

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