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Synthetic Approach for Novel Fluorine Substituted α-Aminophosphonic Acids Containing 1,2,4-Triazin-5-One Moiety as Antioxidant Agents  [PDF]
Mohammed S. T. Makki, Reda M. Abdel-Rahman, Abdulrahman S. Alharbi
International Journal of Organic Chemistry (IJOC) , 2018, DOI: 10.4236/ijoc.2018.81001
Abstract: Novel fluorine substituted α-amino phosphonic acids containing 1,2,4-triazin- 5-one (6a-f) have been obtained from fluoroacylation of 6-(2-amino-5-nitrophenyl)-3-thioxo-1,2,4-triazin-5(4H)-one (1) followed by ammonilysis to give the corresponding 3-amino-derivative 3. Condensation of compound 3 with nitro/halogenated aromatic aldehydes yielded the Schiff bases 4. The simple addition of diethyl phosphonate to compound 4 produced the α-amino phosphonates 5. Acidic hydrolysis of compound 5 produced the fluorine substituted α-amino acids derivatives 6. Structures of the new compounds have been established with the help of elemental analysis and spectral measurements. Also, the products evaluated as antioxidants, where the fluorinated α-amino phosphonic acids 6 are more active than the other synthesized systems.
Synthesis of Fluorinated Heterobicyclic Nitrogen Systems Containing 1,2,4-Triazine Moiety as CDK2 Inhibition Agents  [PDF]
Mohammed Saleh Tawfik Makki, Reda Mohammdy Abdel-Rahman, Faisal Mohammed Aqlan
International Journal of Organic Chemistry (IJOC) , 2015, DOI: 10.4236/ijoc.2015.53020
Abstract: New fluorine substituted heterobicyclic nitrogen system as imidozolopyrimidines (2,3), pyrimido- 1,2,4-triazinones (4-7), 1,2,4-triazinyl-1,2,4-triazine (12-16), 1,2,4-triazinyl-1,2,4-triazinones (14-17) and substituted thiobarbituric acids (19-20), have been synthesized using the reaction of 3- amino-5,6-di (4'-fluorophenyl)-1,2,4-triazine (1) with α,β–bifunctional compounds. Structures of the title compounds were characterized by UV, IR, 1H/13C-NMR and mass spectrometric method. The studied compounds were tested for CDK2 inhibiting activity in DNA damage, as well as in vitro anti-tumor activity.
Synthesis of New Fluorine/Phosphorus Substituted 6-(2’-Amino Phenyl)-3-Thioxo-1,2,4-Triazin-5(2H, 4H)One and Their Related Alkylated Systems as Molluscicidal Agent as against the Snails Responsible for Bilharziasis Diseases  [PDF]
Abeer N. Al-Romaizan, Mohammed S. T. Makki, Reda M. Abdel-Rahman
International Journal of Organic Chemistry (IJOC) , 2014, DOI: 10.4236/ijoc.2014.42017
Abstract: New fluorine substituted 6-(5’-fluoro-2’-triphenylphosphiniminophenyl) 3-thioxo-1,2,4-triazin-5 (2H, 4H) one (2) was obtained via Wittig’s reaction of the corresponding 6-(5’-fluoro-2’-amino-phenyl)-3-thioxo-1,2,4-triazinone (1). Behavior of compound 2 towards alkylating agents and/or oxidizing agents was studied were, N-hydroxyl (3), Mannich base (4,5), S-alkyl (6,7,8) and thiazolo [3,2-b][1,2,4] triazinones (10-14) and or 3-disulfide (18), 3-sulfonic acid 19 and 1,2,4-triazin-3,5-Dionne (20) derivatives obtained. Structures of the new products are established by elemental and spectral data. The new targets obtained screened as Molluscicidalagents against Biomophlaria Alexandrina snails responsible for Bilharziasis diseases, in compare with Baylucide as standard drug.
Synthesis and Antifungal Activity of Some New Fluorine-Substituted 4-Thiazolidinone Bearing 1,2,4-Triazinone  [PDF]
Layla A. Taib
International Journal of Organic Chemistry (IJOC) , 2018, DOI: 10.4236/ijoc.2018.81012
Abstract: Fluorine substituted 4-thiazolidinone 5 bearing 1,2,4-triazinone obtained from the condensation of 3-Amino-6(2’-aminophenyl)-1,2,4-triazin-5(4H)-one (2) with an aromatic aldehyde followed by cycloaddition with mercaptoacetic acid afforded the thiazolidinone (4), and treatment with ethyl trifluoroacetate. Structure of the products has been deduced from their correct elemental analysis and spectral measurements. The antifungal activity of the new fluorinated target also has been evaluated.
Synthesis of New Fluorinated Amino-Heterocyclic Compounds Bearing 6-Aryl-5-Oxo-1,2,4-Triazin-3-Yl Moiety as Antimicrobial Agents  [PDF]
Wafa A. Bawazir, Reda M. Abdel-Rahman
International Journal of Organic Chemistry (IJOC) , 2018, DOI: 10.4236/ijoc.2018.84027
Abstract: Some more new fluorine substitutedamino compounds bearing 6-aryl-5-oxo-1,2,4-triazin-3-yl moieties and its derivatives 3 - 7 have been synthesised successfully from aroylation of 6-(2’-aminophenyl)-3-thioxo-1,2,4-triazin-5-one (1), followed by fluoro amination with 4-fluoroanilinein Abs EtOH and then treated with ammonia/EtOH and finally acylation/aroylation or cyclocondensation reactions with malonic acid in AcOH. Structure of the products has been established upon elemental analysis and their spectral measurements. All the obtained compounds evaluated as antimicrobial agents were the compounds which contained both nitro and fluorine elements and exhibited a highly activity the other derivatives.
Synthesis and Antimicrobial Activity of Some New Pyrazoles, Fused Pyrazolo[3,4-d]-pyrimidine and 1,2-Dihydroimidazo-[2,1-c][1,2,4]triazin-6-one Derivatives  [PDF]
Sobhi Mohamed Gomha,Huwaida M.E. Hassaneen
Molecules , 2011, DOI: 10.3390/molecules16086549
Abstract: A novel series of 7,7-diphenyl-1,2-dihydroimidazo[2,1-c][1,2,4]triazin-6(7H)-one 6a–h, were easily prepared via reactions of novel 2-hydrazinyl-4,4-diphenyl-1H-imidazol-5(4H)-one (2) with hydrazonoyl halides 3a–h. In addition, we also examined the reaction of compound 2 with commercially available active methylene compounds to afford new pyrazoles containing an imidazolone moiety, expected to be biologically active. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, 1H-NMR and mass spectral data. The antifungal and antibacterial activities of the newly synthesized compounds were evaluated.
Fluorine in medicine
Anna Strunecka,Jiri Patocka,Paul Connett
Journal of Applied Biomedicine , 2004,
Abstract: Fluoride has long been known to influence the activity of various enzymes in vitro. Latterly it hasbeen demonstrated that many effects primarily attributed to fluoride are caused by a synergisticaction of fluoride plus aluminum. Fluorinated chemicals are of growing importance, withapplications in medicine. Fluorine substitution has profound effects on the properties of organiccompounds. The very high electronegativity of fluorine can modify electron distribution in themolecule, affecting its absorption, distribution and metabolism. Fluorine-containing drugs are used inmedicine as anesthetics, antibiotics, anti-cancer and anti-inflammatory agents,psychopharmaceuticals, and in many other applications. The potential contribution of fluorinatingpharmaceuticals to human fluoride exposure is discussed.
Synthesis of Some New Fluorine Substituted Thiobarbituricacid Derivatives as Anti HIV1 and Cyclin-Dependent Kinase 2 (CDK2) for Celltumer Division-Part II  [PDF]
Abdulrahman S. Al-Harbi, Reda M. Abdel-Rahman, Abdullah M. Asiri
International Journal of Organic Chemistry (IJOC) , 2014, DOI: 10.4236/ijoc.2014.42016
Abstract: In search for new potential inhibitors some new fluorine substituted thiobarbituric acid derivatives (2-4, 7, 8) and their fused/isolated heterobicyclic nitrogen systems (5, 6, 9, 10, 11, 12) have been synthesized from heterocyclization of fluorinated 1,3-diketoamine (1) with CS2 followed by ring closure reactions with primary nitrogen reagents. Structures of the targets have been established from elemental analysis and spectral data. Some synthesized systems have been evaluated as anti-HIV-1 and of cyclin-dependent kinase 2 (CDK2) for cell tumor division.
Microwave Assisted Synthesis of Some New Fused 1,2,4-Triazines Bearing Thiophene Moieties With Expected Pharmacological Activity  [PDF]
Hosam A. Saad,Mohamed M. Youssef,Mosselhi A. Mosselhi
Molecules , 2011, DOI: 10.3390/molecules16064937
Abstract: Rapid and efficient solvent-free synthesis of 4-amino-3-mercapto-6-[2-(2-thienyl)vinyl]-1,2,4-triazin-5(4H)-one 1 under microwave irradiation is described. Some new fused heterobicyclic nitrogen systems such as 1,2,4-triazino[3,4-b][1,3,4]thiadiazinones, 1,3,4-thiadiazolo[2,3-c][1,2,4]triazinone and pyrazolo[5,1-c]-[1,2,4]triazine-7-carbonitrile, have been synthesized by treatment of 1 with bifunctional oxygen and halogen compounds, CS2/KOH and malononitrile via heterocyclization reactions, in addition to some uncondensed triazines. Structures of the products have been deduced from their elemental analysis and spectral data (IR, 1H-NMR, 13C-NMR). Select new synthesized compounds were screened as anticancer agents, with some showing activity as cytotoxic agents against different cancer cell lines.
5-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene]-2-(4-nitrobenzoyl)-3-phenyl-2,5-dihydro-1,2,4-triazin-6(1H)-one  [PDF]
Darpan Kaushik,Tarawanti Verma
Molbank , 2011, DOI: 10.3390/M733
Abstract: A novel 1,2,4-triazin-6-one derivative ( 2) was synthesized by the reaction of the oxazolone derivative 1 with 4-nitrobenzoic acid hydrazide in the presence of sodium acetate and glacial acetic acid. The title compound 2 was characterized on basis of IR, 1H-NMR, 13C-NMR and mass spectral data.
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