Truncated phosphonated C-1′-branched N,O-nucleosides: A new class of antiviral agents

Romeo, Roberto; Carnovale, Caterina; Giofrè, Salvatore V.; Romeo, Giovanni; Macchi, Beatrice; Frezza, Caterina; Marino-Merlo, Francesca; Pistarà, Venerando; Chiacchio, Ugo

doi:10.1016/j.bmc.2012.03.047

Cited by 29 publications

(18 citation statements)

References 29 publications

(37 reference statements)

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“…flow rate of nitrogen. Consistent with standard procedures, the machine was calibrated for temperature as well as sensitivity with indium [26,27].…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Design and Development of Rilpivirine Nanoparticle Containing Chitosan Using Ionic Gelation Method for Hiv Infections

Patel

2020

Int J Pharm Pharm Sci

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Objective: The primary objective of the current research was to prepare rilpivirine loaded Nanoparticles containing Chitosan using the ionic gelation method for HIV infections. Methods: The nanoparticles of rilpivirine were prepared using the ionic gelation technique. Further, nanoparticles were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and in vitro drug release. Results: The optimized nanoparticles were found with a particle size of 130.30±5.29 nm (mean±SD) and entrapment efficiency (% EE) of 77.10±0.50%. Scanning electron microscopy technique exposed spherical particles with uniform size. It was observed that the nanoparticles created showed the absence of the crystalline nature of the drug and its switch to the amorphous state. Results showed that more than 45% of the pure drug is released in 50 min and after 90 min almost about 95% of the drug is released. Conclusion: The research study concluded that the in vitro release profile of nanoparticles was found to be sustained up to 24 hr. Sustained release of the rilpivirine could improve patient obedience to drug regimens, growing action effectiveness.

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“…flow rate of nitrogen. Consistent with standard procedures, the machine was calibrated for temperature as well as sensitivity with indium [26,27].…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Design and Development of Rilpivirine Nanoparticle Containing Chitosan Using Ionic Gelation Method for Hiv Infections

Patel

2020

Int J Pharm Pharm Sci

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“…NaN 3 (0.36 g, 5.58 mmol) was added to a stirred solution of 1 [14] (0.41 g, 1.12 mmol) in dry DMF (45 mL) under argon at room temperature. The reaction mixture was heated at 90 C for 3 h. The DMF was removed under reduced pressure and the residue was partitioned between H 2 O (50 mL) and Et 2 O (25 mL).…”

Section: Methylmentioning

confidence: 99%

“…Furthermore, 3 0 -deoxy-4 0 -azaribonucleosides have recently shown significant anti-HCV [13] activity and preliminary biological assays on truncated phosphonated C-1 0 -branched N,O-nucleosides show that these systems are able to inhibit HIV infection in vitro [14].…”

Section: Introductionmentioning

confidence: 99%

Synthesis by microwave-assisted 1,3-dipolar cycloaddition of 1,2,3-triazole 1′-homo-3′-isoazanucleosides and evaluation of their anticancer activity

Costa

Garcı́a-Mera

Caamaño

et al. 2015

European Journal of Medicinal Chemistry

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“…Genetic mutation and acquisition of mobile drug resistance genes of microorganisms is a very great resistance and barrier in treating animal and human patients with infectious diseases [4,5]. The importance of the synthesis of novel derivatives of pyridine nucleosides due to their potential use to treat various diseases, such as hepatitis cancer and microbial infections [6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Green Synthesis of Novel 5-Arylazo-2- [(2S, 3S, 4R, 5R)-3, 4, 5- trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yloxy]-4, 6-dimethyl 3-nicotinonitrile.

Mmh¹,

Ah²,

M³

et al. 2017

Chem Sci J

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Green Synthesis of Novel 5-Arylazo-2-[(2S, 3S, 4R, 5R)-3, 4, 5-trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yloxy]-4, 6-dimethyl 3-nicotinonitrile IntroductionPyridine nucleus is one of the most interesting nucleus in organic synthesis. Many uses of pyridines derivatives were investigated in the recent decades especially fluorinated derivatives. One of the recent researches discovered that high tuberculostearic activity of pyridine was observed [1,2].Also from the amazing character of some pyridine is its high fluorescence activities which was used as molecular sensor of picric acid [3].It has been of great importance in the exploring of some novel antimicrobial compounds in veterinary as well as human medicine worldwide. Genetic mutation and acquisition of mobile drug resistance genes of microorganisms is a very great resistance and barrier in treating animal and human patients with infectious diseases [4,5]. The importance of the synthesis of novel derivatives of pyridine nucleosides due to their potential use to treat various diseases, such as hepatitis cancer and microbial infections [6][7][8][9][10].Fluorinated derivatives of pyridines are of high significance in pharmaceutical and medicinal chemistry [11]. Synthesis of poly substituted fluroarylazopyridone by using green protocol is of great effect in synthetic chemistry and also in pharmaceutical chemistry [12]. The presence of fluorine atoms in the molecule can change its lipophilicity, which also affect and change the rate of transportation through lipid membranes [13]. Achievement of green and sustainable chemistry protocol instead of classical methods synthetic chemistry nowadays is of high interest, especially in synthesis of some novel Fluro arylazo pyridine derivatives (1a-e) and their nucleosides (3a-e). Methodology ChemistryGeneral coupling procedures of synthesis of Acetylated -arylazo-2-[(2S, 3S, 4R, 5R)-3, 4, 5-trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yloxy]-4,6dimethylnicotinonitrile AbstractPyridine derivatives played important roles in the last decade in to approach many and different functionalities, especially as antitumor, antibacterial, anti-fungal, and many of pharmacological activities. Novel compounds of 5-Arylazo-2-[(substituted)-3,4,5-trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yloxy]-4,6dimethyl nicotine nitrile, (3a-e), generally called (Fluro arylazo pyridine glucosides) were synthesised via green protocol, microwave scheme 3, and the compounds were investigated on the basis of spectroscopic data (FT-IR, 1D, 13 C), and antibacterial and antifungal studies had been applied. Microwave method: A mixture of 2(1H)-pyridines (1a-e) (10 mmol) and 1″,2″,3″,4″,6″-penta-O-acetyl-α-D-glucopyranose (11 mmol, 4.29 g) where be dissolved in a mixture of methylene chloride/methanol (80/20) then silica gel (200-400 mesh) where be added after that the excess solvent was removed by evaporation. The dried residue was transferred into a 10 mL vial and subjected to microwave irradiation for 2-3 minutes using CEM Microwave syst...

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Truncated phosphonated C-1′-branched N,O-nucleosides: A new class of antiviral agents

Cited by 29 publications

References 29 publications

Design and Development of Rilpivirine Nanoparticle Containing Chitosan Using Ionic Gelation Method for Hiv Infections

Design and Development of Rilpivirine Nanoparticle Containing Chitosan Using Ionic Gelation Method for Hiv Infections

Synthesis by microwave-assisted 1,3-dipolar cycloaddition of 1,2,3-triazole 1′-homo-3′-isoazanucleosides and evaluation of their anticancer activity

Green Synthesis of Novel 5-Arylazo-2- [(2S, 3S, 4R, 5R)-3, 4, 5- trihydroxy-6-(hydroxymethyl) tetrahydro-2H-pyran-2-yloxy]-4, 6-dimethyl 3-nicotinonitrile.

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