Specific phosphorylation of 5-ethyl-2′-deoxyuridine by herpes simplex virus-infected cells and incorporation into viral DNA.

Clercq, Erik De; Bernaerts, R

doi:10.1016/s0021-9258(18)48113-6

Cited by 67 publications

(6 citation statements)

References 28 publications

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“…They can be classified as an important group of annelated uracils having pharmacological significance due to the linkage of the pyrimidine-pyridine system. [37] These compounds are known to have anticancer, [38] antimicrobial, [39] antitubercular, [40] antimalarial [41] and anti-HIV activities. [42] Although the synthesis of pyridopyrimidines is known, the reported procedures face difficulties of multistep synthesis, usage of expensive toxic reagents and solvents, complicated workup procedures and lower yields, [43] which hinder their use in biological applications.…”

Section: Introductionmentioning

confidence: 99%

First‐in‐class pyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones against leishmaniasis and tuberculosis: Rationale, in vitro, ex vivo studies and mechanistic insights

Ramesh

Sarkar

Joji

et al. 2022

Archiv der Pharmazie

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Pyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones were synthesized, for the first time, from indole chalcones and 6‐aminouracil, and their ability to inhibit leishmaniasis and tuberculosis (Tb) infections was evaluated. The in vitro antileishmanial activity against promastigotes of Leishmania donovani revealed exceptional activities of compounds 3, 12 and 13, with IC50 values ranging from 10.23 ± 1.50 to 15.58 ± 1.67 µg/ml, which is better than the IC50 value of the standard drug pentostam of 500 μg/ml. The selectivity of the compounds towards Leishmania parasites was evaluated via ex vivo studies in Swiss albino mice. The efficiency of these compounds against Tb infection was then evaluated using the in vitro anti‐Tb microplate Alamar Blue assay. Five compounds, 3, 7, 8, 9 and 12, showed MIC100 values against the Mycobacterium tuberculosis H37Rv strain at 25 µg/ml, and compound 20 yielded an MIC100 value of 50 µg/ml. Molecular modelling of these compounds highlighted interactions with binding sites of dihydrofolate reductase, pteridine reductase and thymidylate kinase, thus establishing the rationale of their pharmacological activity against both pathogens, which is consistent with the in vitro results. From the above results, it is clear that compounds 3 and 12 are promising lead candidates for Leishmania and Mycobacterium infections and may be promising for coinfections.

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Section: Introductionmentioning

confidence: 99%

First‐in‐class pyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones against leishmaniasis and tuberculosis: Rationale, in vitro, ex vivo studies and mechanistic insights

Ramesh

Sarkar

Joji

et al. 2022

Archiv der Pharmazie

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“…4 Among them, pyrimido[4,5- d ]pyrimidines are very important scaffolds found in many natural products and synthetic drugs or drug candidates exhibiting a wide range of biological activities. 5 These compounds have attracted considerable attention in medicinal chemistry due to their significant and diverse biological activities, including anticancer, 6 antiviral, 7 antifungal, 8 a antioxidant, 8 b antitumor, 9 and hepatoprotective. 10 Some of their derivatives are also useful as bronchodilators, 6 vasodilators, 11 antiallergic, 12 antihypertensive 13 agents.…”

Section: Introductionmentioning

confidence: 99%

TBHP-mediated oxidative synthesis of substituted pyrimido[4,5-d]pyrimidines fromN-uracil amidines and methylarenes under metal free conditions

Debnath

2019

RSC Adv.

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“…14 Furthermore, the pyridopyrimidines are an important class of annelated uracils with biological significance because of their connection with the purine pyridine system. 15 Compounds A and B (Fig. 1) have been found to show adenosine kinase and human neutrophil elastase (HNE) inhibitory activities, respectively.…”

Section: Introductionmentioning

confidence: 99%

Facile synthesis of pyridopyrimidine and coumarin fused pyridine libraries over a Lewis base-surfactant-combined catalyst TEOA in aqueous medium

2013

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A highly convergent and efficient protocol, for the facile synthesis of a library of coumarin fused pyridine and pyridopyrimidine derivatives, has been developed by applying a Lewis basesurfactant-combined catalyst (LBSC) triethanolamine (TEOA). The method described has the benefits of operational simplicity and excellent yields of the targeted molecule. The LBSCs were found to form stable colloidal dispersions rapidly in the presence of reaction substrates in water, even when the substrates are solid.In light of the increased demand for reduction of organic solvents in industry, the surfactant aided Lewis base catalysis described here may have immense practical consequences in organic synthesis. This work may not only lead to environmentally benign systems but also will provide a newer aspect of organic chemistry in water.

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Specific phosphorylation of 5-ethyl-2′-deoxyuridine by herpes simplex virus-infected cells and incorporation into viral DNA.

Cited by 67 publications

References 28 publications

First‐in‐class pyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones against leishmaniasis and tuberculosis: Rationale, in vitro, ex vivo studies and mechanistic insights

First‐in‐class pyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones against leishmaniasis and tuberculosis: Rationale, in vitro, ex vivo studies and mechanistic insights

TBHP-mediated oxidative synthesis of substituted pyrimido[4,5-d]pyrimidines fromN-uracil amidines and methylarenes under metal free conditions

Facile synthesis of pyridopyrimidine and coumarin fused pyridine libraries over a Lewis base-surfactant-combined catalyst TEOA in aqueous medium

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