Synthesis and Antitumor and Antibacterial Properties of New N-Alkylated Pyrimidines

Arutyunyan, A. A.; Mamyan, S. S.; Stepanyan, G. M.; Paronikyan, R. V.

doi:10.1007/s11094-013-0948-8

Cited by 9 publications

(6 citation statements)

References 4 publications

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“…Many uracil based drugs like Sofosbuvir, Trelagliptin, Sparsomycin, Dasabuvir, Zidovudine etc have been developed which possess different functions (Table 1). 5‐fluoro, 5‐iodouracils and 6‐aminouracils are known to have profound antitumour activity [15,16] . The 5‐chloro uracil linked with pyrazolo [1,5‐a][1,3,5] triazines are used as potent thymidine phosphorylase inhibitors [17] .…”

Section: Introductionmentioning

confidence: 99%

“…5-fluoro, 5-iodouracils and 6aminouracils are known to have profound antitumour activity. [15,16] The 5-chloro uracil linked with pyrazolo [1,5a][1, 3,5] triazines are used as potent thymidine phosphorylase inhibitors. [17] Uracil derivatives having thienyl and furanyl moiety displays remarkable activity against herpes simplex virus type 1 (HSV-1) and varicella-zoster virus (VZV).…”

Section: Introductionmentioning

confidence: 99%

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Uracil: A Pharmacophore with Diverse Biological Potential

Jain,

Sharma,

Utreja

2024

ChemistrySelect

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This review article delves into the intricate biological activities of uracil, an essential pyrimidine Base pivotal in RNA structures. Examining its involvement in nucleic acid metabolism, various multifunctional roles, spanning from influencing cell proliferation to its antimicrobial and antiviral properties. The study explores signal transduction pathways affected by uracil, unraveling potential therapeutic applications. By unraveling the nuanced biological mechanisms. This review contributes to a deeper understanding of uracil's impact, offering insights crucial for drug development and advancing biomedical research.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Uracil: A Pharmacophore with Diverse Biological Potential

Jain,

Sharma,

Utreja

2024

ChemistrySelect

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“…In this work, we examine the properties of halogenated uracils. 5-Halouracils (5XU, 1–4 ) are an intriguing class of compounds; such species are cytotoxic yet also have antitumor characteristics, with 5-fluorouracil (5FU, 1 ) being widely used in chemotherapy. − …”

Section: Introductionmentioning

confidence: 99%

Gas-Phase Experimental and Computational Studies of 5-Halouracils: Intrinsic Properties and Biological Implications

Krajewski

Lee

2021

J. Org. Chem.

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The gas-phase acidity and proton affinity (PA) of 5-halouracils (5-fluorouracil, 5-chlorouracil, 5-bromouracil, and 5-iodouracil) have been examined using both theoretical and experimental methods. This work represents a comprehensive study of the thermochemical properties of these nucleobases. Other than 5-fluorouracil acidity, the intrinsic acidity and PA of these halouracils have not been heretofore measured; these new experimental data provide a benchmark for the computational values. Furthermore, we examine these 5-halouracils in the context of the enzyme thymine DNA glycosylase (TDG), which is an enzyme that protects the genome by cleaving these substrates from DNA. Our gas-phase results are compared and contrasted to TDG excision rates to afford insights into the TDG mechanism.

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“…Uracils are used in the area of drug discovery due to their bioactivities, drug similarity in the perspectives of synthetic accessibility and ability. And it is reported that uracils show anti-viral and anti-tumour characteristics in addition to bactericidal, herbicidal and insecticidal features 3 .…”

Section: Introductionmentioning

confidence: 99%

Carbonic anhydrase inhibitory properties of some uracil derivatives

Türkoğlu

Şentürk

Supuran

et al. 2017

Journal of Enzyme Inhibition and Medicinal Chemistry

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Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4–12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The KI values of the compounds 4–12 are in the range of 0.085–428 µM for hCA I and of 0.1715–645 µM against hCA II, respectively. It is concluded from the kinetic investigations, all compounds used in the study act as competitive inhibitors with substrate, 4-NPA. Uracil derivatives are emerging agents for the inhibiton of carbonic anhydrase which could be used in biomedicine.

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Synthesis and Antitumor and Antibacterial Properties of New N-Alkylated Pyrimidines

Cited by 9 publications

References 4 publications

Uracil: A Pharmacophore with Diverse Biological Potential

Uracil: A Pharmacophore with Diverse Biological Potential

Gas-Phase Experimental and Computational Studies of 5-Halouracils: Intrinsic Properties and Biological Implications

Carbonic anhydrase inhibitory properties of some uracil derivatives

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