Publications by authors named "Adel A-H Abdel-Rahman"

29 Publications

  • Page 1 of 1

Genetic polymorphism of fibroblast growth factor receptor 2 and trinucleotide repeat-containing 9 influence the susceptibility to HCV-induced hepatocellular carcinoma.

Clin Res Hepatol Gastroenterol 2021 Mar 16;45(6):101636. Epub 2021 Mar 16.

Tropical Medicine Department, Faculty of Medicine, Menoufia University, Egypt. Electronic address:

Background: Fibroblast growth factor receptor 2 (FGFR2) and trinucleotide repeat-containing 9 (TRNC9) gene polymorphisms have been associated with some cancers. We aimed to assess the association of FGFR2 rs2981582 and TRNC9 rs12443621 polymorphisms with hepatocellular cancer risk.

Methods: One hundred patients with HCV-induced HCC, 100 patients with chronic HCV infection, and 100 controls were genotyped for FGFR2 rs2981582 and TNRC9 rs12443621 using allele-specific Real-Time PCR analysis.

Results: FGFR2 rs2981582 genotype TT was associated with increased risk of HCC when compared to controls (OR = 3.09, 95% CI = 1.24-7.68). However, it was significantly associated with a lower risk of HCC when using HCV patients as controls (OR = 0.21, 95% CI = 0.09-0.5), and T-allele of FGFR2 appears to be a protective allele against HCC in HCV patients (OR = 0.42, 95% CI = 0.21-0.85). While AG and GG genotypes of TNRC9 rs12443621 were linked with significantly increased risk of HCC (OR = 3.91, 95% CI = 2.02-7.6 and OR = 9.26, 95% CI = 3.21-26.7 respectively) and HCV patients carrying G allele were at increased risk of HCC by 2.7-fold. A significant high frequency of small tumor size and early-stage of HCC were observed in patients carrying FGFR2 rs2981582 genotype CT and TT (P = 0.029 and <0.001 respectively), while, TNRC9 rs12443621 genotype AG and GG were associated large tumor size and late-stage of HCC (P < 0.001 and 0.015 respectively).

Conclusions: SNPs in rs2981582 for FGFR2 and rs12443621 for TNRC9 gene were associated with HCC susceptibility, suggesting their implication in hepatocarcinogenesis in chronically HCV-infected patients.
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http://dx.doi.org/10.1016/j.clinre.2021.101636DOI Listing
March 2021

Synthesis and cytotoxic evaluation of novel hybrid estrane heterocycles as chemotherapeutic anti-cancer agents.

Steroids 2021 Feb 27;169:108813. Epub 2021 Feb 27.

Hormones Department, National Research Centre, 12622 Dokki, Giza, Egypt.

New synthesized hybrid steroidal heterocyclic compounds have received a lot of attention in view of their biological activities as anticancer agents. In this study, a novel class of hybrid estrane heterocyclic compounds were synthesized and evaluated by analytical and spectral data which proved the validity of these derivatives. The cytotoxicity of synthesized compounds 2a, 2b, 2c, 3b, 8, 10a, 10b, 13, 14, 16a and 19 against three human cell lines: breast cancer cells (MCF-7), prostate cancer cells (PC3), and liver cancer cells (HepG2) has been tested using MTT assay. Compounds 10a, 10b, 2c, and 14 revealed more inhibitory influence on MCF7, PC3 and HepG2 growth than the reference drug doxorubicin (Dox) after 24 h incubation. Noteworthy, the tested compounds 10a, 10b, 2c, and 14 exhibited the most pronounced effect in this respect. The results were confirmed by morphology study.
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http://dx.doi.org/10.1016/j.steroids.2021.108813DOI Listing
February 2021

Synthesis and Antibacterial Activities of Different Five-Membered Heterocyclic Rings Incorporated with Pyridothienopyrimidine.

ACS Omega 2020 Mar 10;5(11):6163-6168. Epub 2020 Mar 10.

Basic Science Department, Preparatory Year Deanship, Prince Sattam Bin Abdulaziz University, Al Kharj 16278, Saudi Arabia.

Certain pyridothienopyrimidine derivatives exhibit antiatheroscleorotic, antibacterial, antiviral, antidepressant, antidiabetic, antihypertensive, anticancer, antihistaminic, antiallergic, anti-inflammatory, spasmolytic, analgesic, and neurotropic activities. 4-Hydrazino-7,9-dimethylpyrido[3',2':4,5]thieno[3,2-]pyrimidine () is a reported pyridothienopyrimidine derivative. In the current study, () has been reacted with different reagents to obtain 12 new pyridothienopyrimidine derivatives. The newly synthesized five-membered heterocyclic rings incorporated with pyridothienopyrimidines have been screened for their antibacterial activities. The results encourage further studies on other possible biological activities.
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http://dx.doi.org/10.1021/acsomega.0c00188DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7098019PMC
March 2020

Synthesis and Cytotoxic Activity of New Thiazolopyrimidine Sugar Hydrazones and Their Derived Acyclic Nucleoside Analogues.

Molecules 2020 Jan 18;25(2). Epub 2020 Jan 18.

Photochemistry Department, National Research Centre, Giza 12511, Egypt.

New thienyl- or chlorophenyl-substituted thiazolopyrimidine derivatives and their derived sugar hydrazones incorporating acyclic d-galactosyl or d-xylosyl sugar moieties in addition to their per-O-acetylated derivatives were synthesized. Heterocyclization of the formed sugar hydrazones afforded the derived acyclic nucleoside analogues possessing the 1,3,4-oxadiazoline as modified nucleobase via acetylation followed by the cyclization process. The cytotoxic activity of the synthesized compounds was studied against human breast cancer MCF7 and MDA-MB-231 cell lines as well as human colorectal cancer HCT 116 and Caco-2 cell lines. High activities were revealed by compounds , , , , and against Caco-2 and MCF7 cells in addition to moderate activities exhibited by other compounds against HCT116 or MDA-MB-231 cells.
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http://dx.doi.org/10.3390/molecules25020399DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7024276PMC
January 2020

cuticle glycoproteins in the diagnosis of calves' toxocariasis.

Vet World 2019 20;12(2):288-294. Epub 2019 Feb 20.

Department of Parasitology and Animal Diseases, National Research Centre, Giza, Egypt.

Aim: The current study was designed to isolate and characterize glycoprotein antigens and then to evaluate its potency in accurate diagnosis of toxocariasis.

Materials And Methods: glycoprotein fractions were isolated using Con-A affinity chromatography. The fractions characterized using sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), and immunoblot assay. Mass spectrometric analysis was used for identification of proposed structure of the N-acetylglucosamine (GlcNAc) fraction. Enzyme-linked immunosorbent assay (ELISA) was used to assess the diagnostic potential of the isolated fractions.

Results: Surface of adult worm revealed two glycoprotein fractions rich in glucose (Glc) and GlcNAc. Three bands of molecular weight 212kDa, 107 kDa, and 93 kDa were detected in Glc fraction by SDS-PAGE. These bands were also detected in GlcNAc fraction with an additional band of 49 kDa. GlcNAc fraction showed more diagnostic potency of calves' toxocariasis; 79% than Glc fraction; 46.9% by indirect ELISA. The additional band of 49 kDa in GlcNAc fraction is probably responsible for its higher diagnostic potentials. Western blotting verified the immunoreactivity of the Glc and GlcNAc isolated fraction as they reacted with calves sera infected with toxocariasis. The proposed structure of GlcNAc fraction was Ser-Meth-Arg-O-methylated GlcNAc.

Conclusion: GlcNAc-rich fraction of can be successfully utilized in the diagnosis of calves' toxocariasis.
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http://dx.doi.org/10.14202/vetworld.2019.288-294DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6460866PMC
February 2019

Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides.

Mini Rev Med Chem 2019 ;19(13):1093-1110

Chemistry Department, Faculty of Science, Qassim University, Buraydah, Saudi Arabia.

Background & Objective: New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.

Methods: The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.

Results: The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.

Conclusion: Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior.
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http://dx.doi.org/10.2174/1389557519666190312165717DOI Listing
October 2019

Synthesis and Evaluation of Novel Cholestanoheterocyclic Steroids as Anticancer Agents.

Appl Biochem Biotechnol 2019 Jul 6;188(3):635-662. Epub 2019 Jan 6.

Hormones Department, National Research Centre, Dokki, Giza, 12622, Egypt.

Modification of steroid molecules by introducing heterocyclic ring into the core structure of steroids has been utilized as an attractive approach for either cancer prognosis or diagnosis. Several new cholestanoheterocyclic steroids were synthesized, and analytical and spectral data proved the validity of the novel synthesized steroid derivatives. The cytotoxicity of synthesized compounds 3, 4, 5, 7, 9, 10, 13, 15b, and 16b was evaluated using human colorectal cancer HCT 116 and Caco-2, cervical cancer HeLa, hepatoma HepG2, and breast cancer MCF7 cell lines. Intriguingly, compound 13 has the highest cytotoxic effect when applied on the majority of cancer cells. In conclusion, compound 13 may be considered as a promising anticancer candidate against all cancer cell lines, because it recorded the lowest IC of the majority of the cancer cell lines used. Furthermore, a molecular docking study was employed to determine the binding modes against aromatase cytochrome P450 (CYP19), cyclin-dependent kinase 2 (CDK2), and B-cell lymphoma (BCL-2) proteins, which are major proteins involved in the pathogenesis of cancer. Molecular docking analyses revealed that compounds 13, 3, and 5 (free energy of binding = - 9.2, - 9.1, and - 9.0 kcal/mol, respectively) were the best docked ligand against aromatase CYP19; compounds 16b, 3, 9, and 10 (free energy of binding = - 9.6, - 9.3, and - 9.2 kcal/mol, respectively) were the best docked ligand against CDK2, while compounds 15b, 16b, and 13 (free energy of binding = - 9.1, - 9.0, and- 8.7 kcal/mol, respectively) were the best docked ligand against BCL2. In conclusion, compounds 3, 13, and 16b were the most promising compounds with the lowest ICs against most of the tested cancer cell lines, and they displayed the lowest binding energies, critical hydrogen bonds, and hydrophobic interactions with the three molecular targets compared to other tested compounds.
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http://dx.doi.org/10.1007/s12010-018-02943-6DOI Listing
July 2019

Functionalization of Magnetic Chitosan Particles for the Sorption of U(VI), Cu(II) and Zn(II)-Hydrazide Derivative of Glycine-Grafted Chitosan.

Materials (Basel) 2017 May 16;10(5). Epub 2017 May 16.

Ecole des Mines d'Alès, Centre des Matériaux des Mines d'Alès, 6 Avenue de Clavières, F-30319 Ales CEDEX, France.

A new magnetic functionalized derivative of chitosan is synthesized and characterized for the sorption of metal ions (environmental applications and metal valorization). The chemical modification of the glycine derivative of chitosan consists of: activation of the magnetic support with epichlorohydrin, followed by reaction with either glycine to produce the reference material (i.e., Gly sorbent) or glycine ester hydrochloride, followed by hydrazinolysis to synthesize the hydrazide functionalized sorbent (i.e., HGly sorbent). The materials are characterized by titration, elemental analysis, FTIR analysis (Fourrier-transform infrared spectrometry), TGA analysis (thermogravimetric analysis) and with SEM-EDX (scanning electron microscopy coupled to energy dispersive X-ray analysis). The sorption performances for U(VI), Cu(II), and Zn(II) are tested in batch systems. The sorption performances are compared for Gly and HGly taking into account the effect of pH, the uptake kinetics (fitted by the pseudo-second order rate equation), and the sorption isotherms (described by the Langmuir and the Sips equations). The sorption capacities of the modified sorbent reach up to 1.14 mmol U g, 1.69 mmol Cu g, and 0.85 mmol Zn g. In multi-metal solutions of equimolar concentration, the chemical modification changes the preferences for given metal ions. Metal ions are desorbed using 0.2 M HCl solutions and the sorbents are re-used for five cycles of sorption/desorption without significant loss in performances.
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http://dx.doi.org/10.3390/ma10050539DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5459025PMC
May 2017

The role of Ser-(Arg-Ser-Arg-Ser-GlucNAc)19-GlucNAc Fasciola gigantica glycoprotein in the diagnosis of prepatent fasciolosis in rabbits.

J Parasit Dis 2016 Mar 26;40(1):11-21. Epub 2014 Apr 26.

Department of Parasitology and Animal Diseases, National Research Center, Giza, Egypt.

In the present study, the carbohydrate structures associated with Fasciola gigantica adult worm were identified by indirect hemagglutination inhibition test. Glucose was found to be the main monosaccharide associated with the fluke. According to indirect hemagglutination inhibition results, purification of glycoprotein fractions from worm crude extract was carried out by affinity chromatography immobilized glucose agarose gel and Con-A lectin columns. The isolated glycoprotein fractions, FI and FII, were characterized by SDS-PAGE which revealed one band in FI of 26 kDa and another one band of 19.5 kDa in FII compared with 12 bands associated with whole worm extract. Both fractions were also characterized by isoelectric focusing technique which proved that both bands were acidic in nature with pIs 6.4 and 6.5 respectively. The comparative diagnostic evaluation of the two isolated glycoprotein fractions and crude extract of experimental fasciolosis in rabbits by ELISA revealed that FII was more potent in the diagnosis during prepatent (first week post infection) and patent periods (10 weeks post infection) than FI and crude extract. Moreover, infected rabbit sera at ten weeks post infection identified both bands; 26 and 19.5 kDa in western blot analysis confirming its immunodiagnostic activities which was proved previously by ELISA. FII proved potency in diagnosis of fasciolosis in 200 buffalo serum samples of different ages and sexes using ELISA which recorded 95 % positive and 5 % negative samples. Moreover, the detailed structural analyses of the most potent fraction, F11, using mass spectrum was made and elucidated chemical structure; O-glycan [Ser-(Arg-Ser-Arg-Ser-GlucNAc)19-GlucNAc]. The present result introduces GlucNAc rich fraction of F .gigantica that can be used successfully in the diagnosis of acute and chronic fasciolosis.
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http://dx.doi.org/10.1007/s12639-014-0461-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4815834PMC
March 2016

Synthesis and antiviral evaluation of alpha-amino acid esters bearing N6-benzyladenine side chain.

Acta Pol Pharm 2012 Sep-Oct;69(5):917-25

Department of Applied Chemistry, Faculty of Applied Science, Taibah University, Madinah, Saudi Arabia.

A series of peptide derivatives conjugated with a purine residue were synthesized. The prepared compounds were tested for antiviral activity against Hepatitis B Virus (HBV) displaying different degrees of antiviral activities or inhibitory actions.
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November 2012

Repellent and insecticide activity of Pelargonium x hortorum against Spodoptera littoralis (Boisd.).

Z Naturforsch C J Biosci 2012 Jul-Aug;67(7-8):398-404

Department of Pest Physiology, Plant Protection Research Institute, Agricultural Research Center, Dokki, Giza, Egypt.

Insecticide and repellent activity of an acetone extract and oil from fresh leaves of Pelargonium x hortorum (cv. Orangesonne) were evaluated against the 2nd and 4th instar larvae of Spodoptera littoralis (Boisd.) (Lepidoptera: Noctuidae). The oil showed medium toxicity against the 2nd instar and low toxicity against the 4th instar larvae, while the extract showed high significant toxicity at all concentrations tested against the two instars. On the other hand, both oil and extract exhibited highly significant repellency against the two tested instars. Volatile constituents of the oil were also identified by GC-MS analysis.
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http://dx.doi.org/10.1515/znc-2012-7-807DOI Listing
October 2012

Anticancer activity of new (tetrazol-5-yl)methylindole derivatives and their acyclic c-nucleoside analogs.

Acta Pol Pharm 2012 Jul-Aug;69(4):669-77

Department of Photochemistry, National Research Centre, Cairo, Egypt.

New (tetrazol-5-yl)methylindole derivatives were synthesized from 2-phenylindole. Furthermore, the sugar acetyl hydrazones of the tetrazole derivatives as well as their derived acyclic C-nucleoside analogs were prepared. The synthesized compounds were studied for their anticancer activity against human liver carcinoma cell line (HepG2) and the results showed that arylidine substituted tetrazole derivatives 7c and 7d were the most active.
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August 2012

Antimicrobial activity of new synthesized [(oxadiazolyl)methyl]phenytoin derivatives.

Acta Pol Pharm 2012 Jul-Aug;69(4):657-67

Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Koam, Egypt.

A number of substituted phenytoin derivatives in addition to their sugar hydrazones were newly synthesized. Furthermore, the corresponding derived 1,3,4-oxadiazole and their thioglycoside as well as their acyclic analogs were prepared. The antimicrobial activity of the prepared compounds was evaluated against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Aspergillus niger and Candida albicans. The dithiohydrazone as well as oxadiazole thiole derivatives, sugar hydrazones and acyclic nucleoside analogs were the highly active compounds.
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August 2012

Antitumor and antimicrobial activities of some hetero aromatic benzofurans derived from naturally occurring visnagin.

Acta Pol Pharm 2012 Jul-Aug;69(4):645-55

Natural Products Department, National Research Center, Dokki, Cairo, Egypt.

Bromination of visnaginone (1) yielded the dibromo derivative (2), which upon methylation with methyl iodide gave 1-(2,7-dibromo-4,6-dimethoxybenzofuran-5-yl) ethanone (3). Compound (3) reacted with dimethylformamide dimethylacetal to give (4). The reaction of (3) with aromatic aldehydes namely (vanillin, benzaldehyde and 3-anisaldehyde) in ammonium acetate, malononitrile and/or butyric cyanoanhydride gave the 2-amino substituted nicotinonitriles (5a-c) and the 2-hydroxyl substituted nicotinonitriles (7a-c), respectively, while in piperidine gave (E)-1-(2,7-dibromo-4,6-dimethoxybenzofuran-5-yl)-3-(substituted)prop-2-en-l-one (11a-c). (5a) was hydrolyzed with sulfuric acid on cold to give the nicotinic acid derivative (6a). When compound (3) reacted with hydrazines and aromatic amines, it gave the Schiff bases (8a,b) and (10a,b), respectively. (8b) reacted with thioglycolic acid to give the thiazolidin-4-one (9b). When (11a-c) reacted with thiourea, it gave the pyrimidine derivatives (12a-c). (11a,b) also reacted with butyric cyanoanhydride and hydroxylamine hydrochloride to give (13a,b) and (15a,b), respectively. When the carboxylate (13a) was treated with 2,4-dinitroaniline, it gave the carboxamide (14a). Compounds (11b,c) reacted with hydrazine derivatives (hydrazine hydrate and phenylhydrazine) yielding the substituted pyrazole derivatives (16b,c) and (17b,c), respectively. All the structures of the synthesized compounds were elucidated by elemental analyses and spectral data. The newly synthesized benzofuran compounds showed a strong to moderate cytotoxicity against liver HEPG2 cancer cell line compared to 5-fluorouracil and doxorubicin (the anticancer agents). Compounds (2, 6a, 13a, 14a, 16c and 17b) were the most active compounds in descending order. The synthesized compounds were also tested for their antimicrobial activity. Compound (10b) showed the highest activity against all the tested strains followed by 6, 10a, 5a, 8b and 7a in descending order.
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August 2012

Synthesis and antimicrobial activity of new substituted thienopyrimidines, their tetrazolyl and sugar derivatives.

Acta Pol Pharm 2012 May-Jun;69(3):439-47

Department of Chemistry, Faculty of Science, NBU University, Kingdom of Saudi Arabia.

A series of substituted 5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d]pyrimidine-4-one derivatives were newly synthesized starting from 5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d]pyrimidine-4-one derivatives (1). Furthermore, their derived tetrazolyl as well as the N-substituted derivatives were also prepared. The antimicrobial activity of the prepared compounds against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Aspergillus niger and Candida albicans were evaluated. The substituted thienopyrimidine derivatives 4 and 6 as well as the arylidine 10 were the highly active compounds.
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July 2012

Repellent and insecticidal activities of Melia azedarach L. against cotton leafworm, Spodoptera littoralis (Boisd.).

Z Naturforsch C J Biosci 2011 Mar-Apr;66(3-4):129-35

Department of Pest Physiology, Plant Protection Research Institute, Agricultural Research Center, Dokki, Giza, Egypt.

A crude acetone extract and oil of ripe fruits from Melia azedarach L. were evaluated against the 2nd and 4th instar larvae of Spodoptera littoralis (Boisd.) (Lepidoptera: Noctuidae). Both oil and extract exhibited highly significant growth inhibition at all concentrations tested, while the oil of M. azedarach recorded higher insecticidal activity against both instars than the crude extract. GC-MS analysis of the oil revealed the presence of linoleic acid methyl ester, oleic acid methyl ester, and free oleic acid as the main components in addition to hexadecanol, palmitic acid, methyl esters of stearic acid and myristic acid. Fatty acids and their esters were not only the main constituents of essential oil from the ripe fruits of M. azedarach, but also mainly responsible for the insecticidal and growth inhibition activity against S. littoralis.
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http://dx.doi.org/10.1515/znc-2011-3-406DOI Listing
June 2011

Antimicrobial activity of new 4,6-disubstituted pyrimidine, pyrazoline, and pyran derivatives.

Arch Pharm Res 2010 May 29;33(5):647-54. Epub 2010 May 29.

Department of Physics and Mathematical Engineering, Menoufia University, Menouf, Egypt.

A number of new 2,6-didisubstituted pyrimidine, pyrazoline, and pyran derivatives were synthesized starting from their chalcone derivative. The synthesized compounds displayed different degrees of antimicrobial activity against Bscillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes).
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http://dx.doi.org/10.1007/s12272-010-0501-1DOI Listing
May 2010

Synthesis and antimicrobial activity of new substituted fused 1,2,4-triazole derivatives.

Z Naturforsch C J Biosci 2010 Jan-Feb;65(1-2):22-8

Photochemistry Department, National Research Centre, Cairo, Egypt.

A number of new substituted 1,2,4-triazole, 1,2,4-triazolo[3,4-b]1,3,4-thiadiazole and 1,2,4-triazolo[3,4-b]1,3,4-thiadiazine derivatives were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). The synthesized compounds displayed different degrees of antimicrobial activities or inhibitory actions.
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http://dx.doi.org/10.1515/znc-2010-1-204DOI Listing
April 2010

Synthesis and antimicrobial activity of new substituted 1,2,4-triazoles and their acyclic C-nucleoside analogues.

Z Naturforsch C J Biosci 2010 Jan-Feb;65(1-2):15-21

Photochemistry Department, National Research Centre, Cairo, Egypt.

A number of new substituted 1,2,4-triazole {[(1,2,4-triazolyl)ethyl]tetrazolyl} derivatives, their sugar hydrazones, and their acyclic C-nucleoside analogues were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). The synthesized compounds displayed different degrees of antimicrobial activities or inhibitory actions.
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http://dx.doi.org/10.1515/znc-2010-1-203DOI Listing
April 2010

Antimicrobial activity of new 2,4-disubstituted thiazolidinone derivatives.

Z Naturforsch C J Biosci 2009 Nov-Dec;64(11-12):785-9

Photochemistry Department, National Research Center, El Dokki, Cairo, Egypt.

A number of new disubstituted 2,5-thiazolidinone derivatives were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). They displayed different degrees of antimicrobial activities or inhibitory actions.
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http://dx.doi.org/10.1515/znc-2009-11-1205DOI Listing
April 2010

Anti-HIV activity of new substituted 1,3,4-oxadiazole derivatives and their acyclic nucleoside analogues.

Z Naturforsch C J Biosci 2009 Nov-Dec;64(11-12):773-8

Photochemistry Department, National Research Center, El Dokki, Cairo, Egypt.

A number of new 5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazole derivatives, 2-5 and 8-11, were synthesized. The 2-{5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazol-2-ylthio}acetohydrazones 6a and 6b were synthesized by the reaction of the hydrazide 4 with the corresponding monosaccharides. Cyclization of the sugar hydrazones 6a and 6b with acetic anhydride afforded the substituted oxadiazoline derivatives 7a and 7b. The synthesized compounds were evaluated for their antiviral activity against, the human immunodeficiency virus (HIV-1) and some of these compounds showed moderate to high antiviral activity.
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http://dx.doi.org/10.1515/znc-2009-11-1203DOI Listing
April 2010

Anti-hepatitis B virus activity of new substituted pyrimidine acyclic nucleoside analogues.

Z Naturforsch C J Biosci 2009 Nov-Dec;64(11-12):767-72

Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Koam, Egypt.

A number of N-substituted pyrimidine acyclic nucleosides were synthesized by coupling reaction of 2-(2-chloroethoxy)ethyl acetate or (2,2-dimethyl-1,3-dioxolan-4-yl)methyl 4-methylbenzenesulfonate with the corresponding base followed by deprotection. The synthesized compounds were tested for their antiviral activity against hepatitis B virus (HBV). The plaque reduction infectivity assay was used to determine virus count reduction as a result of treatment with the synthesized compounds which showed moderate to high antiviral activities.
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http://dx.doi.org/10.1515/znc-2009-11-1202DOI Listing
April 2010

Anti-hepatitis B virus activity of new N4-beta-D-glycoside Pyrazolo [3,4-d]pyrimidine derivatives.

Z Naturforsch C J Biosci 2009 May-Jun;64(5-6):323-8

Photochemistry Department, National Research Center, El Dokki, Cairo, Egypt.

The reaction of 6-hydrazinyl-1,3-dimethylpyrimidine-2,4-(1H,3H)-dione (1) with ethoxymethylenemalononitrile afforded 5-amino-1-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-6-yl)-1H-pyrazole-4-carbonitrile (2). The latter was reacted with formamide and urea affording the corresponding 4-aminopyrazolo[3,4-d]pyrimidines 3 and 4. The reaction of monosaccharide aldoses with 3 and 4 gave stereoselectively the beta-N-glycosides 5a-d and 6a-d which were treated with acetic anhydride in pyridine to afford the corresponding acetylated derivatives 7a-d and 8a-d. The prepared compounds were tested for their antiviral activity against hepatitis B virus (HBV) and showed moderate to high activities.
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http://dx.doi.org/10.1515/znc-2009-5-603DOI Listing
September 2009

Synthesis and antiviral evaluation of 5-(1,2,3-triazol-1-ylmethyl)uridine derivatives.

Z Naturforsch C J Biosci 2009 Mar-Apr;64(3-4):163-6

Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Koam, Egypt.

Some 5-(1,2,3-triazol-1-ylmethyl)uridine derivatives were synthesized via the 1,3-dipolar cycloaddition of a 5-azidomethyluridine derivative with substituted acetylenes. The antiviral activities of these compounds against hepatitis A virus (HAV, MBB cell culture-adapted strain) and Herpes simplex virus type-1 (HSV-1) were tested.
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http://dx.doi.org/10.1515/znc-2009-3-402DOI Listing
July 2009

Anti-hepatitis B virus activity of new pyrimidine and adenine peptide nucleic acid analogues.

Z Naturforsch C J Biosci 2009 Jan-Feb;64(1-2):6-10

Chemistry Department, Faculty of Science, Menofia University, Shebin El-Koam, Egypt.

A number of N-substituted thymine and adenine derivatives, 2a, b and 3a, b, were synthesized by the coupling reaction of 1-bromo-2,2-diethoxyethane with the corresponding base. The corresponding peptide nucleic acid (PNA) analogues, N-substituted ethylamino-3-hydroxypropanoate derivatives 5a, b and ethylamino-3-hydroxybutanoate derivatives 6a, b, were synthesized from the corresponding 2-[3,4-dihydro-5-methyl-2,4-dioxopyrimidin-1(2H)-yl]-acetaldehyde (3a) and 2-[6-amino-4H-purin-9(5H)-yl]-acetaldehyde (3b), respectively. The synthesized compounds were tested for their antiviral activity against hepatitis B virus (HBV). The plaque reduction infectivity assay was used to determine the virus count reduction as a result of the treatment with the tested compounds.
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http://dx.doi.org/10.1515/znc-2009-1-202DOI Listing
April 2009

Synthesis and antiviral evaluation of novel 2,3-dihydroxypropyl nucleosides from 2- and 4-thiouracils.

Nucleosides Nucleotides Nucleic Acids 2008 Dec;27(12):1257-71

Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Koam, Egypt.

Regioselective alkylation of 2-thiouracils 1a-c and 4-thiouracils 7a,b with 2,3-O-isopropylidene-2,3-dihydroxypropyl chloride (2) afforded 2-[[(2,2-Dimethyl-1,3-dioxolan-4-yl) methyl]thio]pyrimidin-4(1H)-ones 3a-c and 4-[[(2,2-Dimethyl-1,3-dioxolan-4-yl)methyl]thio] pyrimidin-2(1H)-ones 8a,b, respectively. Further alkylation with 2 and/or 2,3-O-isopropylidine-1-O-(4-toluenesulfonyl)-glycerol (4) gave the acyclo N-nucleosides 5a-c and 9a,b whose deprotection afforded 6a-c and 10a,b. 2-(Methylthio)pyrimidin-4(1H)-ones 11a-c and 4-(methylthio)pyrimidin-2(1H)-ones 14a,b were treated with 2 and/or 4 to give 12a-c and 15a,b which were deprotected to give 13a-c and 16a,b. Pyrimidine-2,4(1H,3H)-dithiones 17a-c were treated with two equivalents of 2 to give 2,4-bis[[(2,2-dimethyl-1,3-dioxolan-4-yl)methyl]thio] pyrimidines 18a-c. Deprotection of compounds 18a-c gave 2,4-bis[(2,3-dihydroxypropyl)thio]pyrimidines 19a-c. The activity of the deprotected nucleosides against Hepatitis B virus was evaluated and showed moderate inhibition activity against HBV with mild cytotoxicity.
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http://dx.doi.org/10.1080/15257770802086898DOI Listing
December 2008

Synthesis and anti-HBV activity of thiouracils linked via S and N-1 to the 5-position of methyl beta-D-ribofuranoside.

Nucleosides Nucleotides Nucleic Acids 2003 Nov;22(11):2027-38

Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Koam, Egypt.

Reverse nucleoside derivatives of 2-(methylsulfanyl)uracils 6a-d were prepared by treating of the sodium salt of 2-(methylsulfanyl)uracils (5a-d) with methyl 2,3-O-isopropylidene-5-O-p-toluenesulfonyl-beta-D-ribofuranoside (2). The alkylation of 2-thiouracils 4a-d with methyl 5-deoxy-5-iodo-2,3-O-isopropylidene-D-ribofuranoside (3) afforded the corresponding S-ribofuranoside derivatives 8a-d. Deisopropylidenation of 6a-d and 8a-d afforded the corresponding deprotected derivatives 7a-d and 9a-d, respectively. The Anti-HBV activity of selected compounds was studied.
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http://dx.doi.org/10.1081/NCN-120026404DOI Listing
November 2003

Efficient intramolecular beta-mannoside formation using m-xylylene and isophthaloyl derivatives as rigid spacers.

Carbohydr Res 2002 Feb;337(3):195-206

Department of Chemistry, University of Konstanz, Fach M 725, D-78457, Konstanz, Germany.

A series of mannosyl donors linked via position 2 to an m-xylylene or an isophthaloyl spacer which was connected to the position 6 of a glucoside acceptor afforded, via intramolecular glycosylation, the corresponding disaccharides with high beta anomeric ratio.
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http://dx.doi.org/10.1016/s0008-6215(01)00306-8DOI Listing
February 2002