Ecofriendly microwave assisted synthesis of some new pyridine glycosides

Eldeab, Hany A.

doi:10.1080/15257770.2018.1562075

Cited by 5 publications

(3 citation statements)

References 19 publications

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“…One of the most important strategies in structure-based drug design, is molecular docking, as it can give an idea of the binding modes of the novel molecules in the binding site of the suitable target, which is a key step in drug design [36,37]. In this research work, docking studies were performed to give insight into the mode of binding between the enzyme active binding site and the novel bioactive compound, in addition to possible interactions and the docking score.…”

Section: Resultsmentioning

confidence: 99%

Synthesis, Docking Studies, and In Vitro Evaluation of Some Novel Thienopyridines and Fused Thienopyridine–Quinolines as Antibacterial Agents and DNA Gyrase Inhibitors

et al. 2019

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A series of novel thienopyridines and pyridothienoquinolines (3a,b–14) was synthesized, starting with 2-thioxo-1,2-dihydropyridine-3-carbonitriles 1a and 1b. All compounds were evaluated for their in vitro antimicrobial activity against six bacterial strains. Compounds 3a,b, 4a, 5b, 6a,b, 7a, 9b, 12b, and 14 showed significant growth inhibition activity against both Gram-positive and Gram-negative bacteria compared with the reference drug. The most active compounds (4a, 7a, 9b, and 12b) against Staphylococcus aureus were also tested for their in vitro inhibitory action on methicillin-resistant Staphylococcus aureus (MRSA). The tested compounds showed promising inhibition activity, with the performance of 12b being equal to gentamicin and that of 7a exceeding it. Moreover, the most promising compounds were also screened for their Escherichia coli DNA gyrase inhibitory activity, compared with novobiocin as a reference DNA gyrase inhibitor. The results revealed that compounds (3a, 3b, 4a, 9b, and 12b) had the highest inhibitory capacity, with IC50 values of 2.26–5.87 µM (that of novobiocin is equal to 4.17 µM). Docking studies were performed to identify the mode of binding of the tested compounds to the active site of E. coli DNA gyrase B.

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Section: Resultsmentioning

confidence: 99%

Synthesis, Docking Studies, and In Vitro Evaluation of Some Novel Thienopyridines and Fused Thienopyridine–Quinolines as Antibacterial Agents and DNA Gyrase Inhibitors

et al. 2019

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“…Microwave synthetic methods (methods A and B) were used as simple, efficient approaches to the preparation of the targeted galactosides (8 a–d ) and (11 a–c ) in a limited time with an excellent yield. In method A, the solvent-free reaction was conducted using microwave irradiation to enhance the reaction between the routine pyridine-2(1 H )-ones ( 3 a–d , 10 a–c ) and 1″,2″,3″,4″,6″-penta- O -acetyl-α- d -galactopyranose ( 6 ) in the presence of a catalyst [21] to afford the 3-cyano-2-(2″,3″,4″,6″-tetra- O -acetyl-β- d -galactopyranosyloxy) pyridines ( 8 a–d ) and ( 11 a–c ) in high yields (87–95%). The same galactosides ( 8 a–d ) and ( 11 a–c ) were obtained in better yields utilizing the pyridinium salts ( 4 a–d , 13 a–c ) and (2″,3″,4″,6″-tetra- O -acetyl-α- d -galactopyranosyl bromide) ( 7 ) (in dry acetone/DMF without any catalyst under microwave irradiation).…”

Section: Resultsmentioning

confidence: 99%

“…Molecular docking is one of the most preferred methods in structure-based drug design, as it gives a good exploration into the binding mode of the new small molecules in the binding site of their appropriate targets. Understanding binding behavior is a key step in rational drug design [21,22]. Docking studies were performed in this research work to give insight into possible interactions, the docking score, and the mode of binding between the enzyme active binding site and the new bioactive molecules.…”

Section: Resultsmentioning

confidence: 99%

An Eco-Friendly Technique: Solvent-Free Microwave Synthesis and Docking Studies of Some New Pyridine Nucleosides and Their Pharmacological Significance

et al. 2019

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Two series of novel 5-arylazo-3-cyano-2-(2″,3″,4″,6″-tetra-O-acetyl-β-d-galacto pyranosyloxy) pyridines and 3-cyano-2-(2″,3″,4″,6″-tetra-O-acetyl-β-d-galactopyranosyloxy) pyridines were synthesized in high yields utilizing a microwave-assisted synthesis tool guided by the principles of green chemistry. The chemical structures of the new substances were confirmed on the basis of their elemental analysis and spectroscopic data (FT-IR, 1D, 2D-NMR). Activity against different bacterial strains was studied. The anticancer potential of the new compounds is also discussed. Molecular docking was used as a tool in this research work to get better insight into the possible interactions, affinities, and expected modes of binding of the most promising derivatives of the potential chemotherapeutic target (DHFR).

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New thieno[2,3-b]pyridine-based compounds: Synthesis, molecular modelling, antibacterial and antifungal activities

Alenazi,

Alharbi,

Fawzi Qarah

et al. 2023

Arabian Journal of Chemistry

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Ecofriendly microwave assisted synthesis of some new pyridine glycosides

Cited by 5 publications

References 19 publications

Synthesis, Docking Studies, and In Vitro Evaluation of Some Novel Thienopyridines and Fused Thienopyridine–Quinolines as Antibacterial Agents and DNA Gyrase Inhibitors

Synthesis, Docking Studies, and In Vitro Evaluation of Some Novel Thienopyridines and Fused Thienopyridine–Quinolines as Antibacterial Agents and DNA Gyrase Inhibitors

An Eco-Friendly Technique: Solvent-Free Microwave Synthesis and Docking Studies of Some New Pyridine Nucleosides and Their Pharmacological Significance

New thieno[2,3-b]pyridine-based compounds: Synthesis, molecular modelling, antibacterial and antifungal activities

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