Synthesis of Some New Fluorine Substituted Thiobarbituricacid Derivatives as Anti HIV1 and Cyclin-Dependent Kinase 2 (CDK2) for Celltumer Division-Part II

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.

Synthesis and Characterization of Some Transition Metal Chelates of 5-(1-Hydroxy-6-Naphthylazo-3-Sodium Sulphonate) Thiobarbituric (L_1) and Barbituric (L_2) Acids

Some transition metal chelates of two ligands L1 and L2 were prepared and characterized by elemental analysis. The IR and 1H NMR spectra of several chelates of two ligands L1 and L2 showed the involvement of the azo group in chelation with the transition metaI ions, in most of the studied chelates, and that the two ligands L1 and L2 showed the involvement of the azo group in chelation with the transition metal ions, in most of the studied chelates, and that the two ligands L1 and L2 were coordinated either in the enol or the keto form. IR spetra also showed that Fe(III)-, Ni(II)-, Mn(II)-, VO(II)-L1 and Cu(II)-L2 chelates behaved in a bidentate manner, in contrast with the two (1:1) M:L cobalt chelates with the two ligands are tridentate.TG analysis indicated the presence of three to twelve water molecules of hydration eliminated on heating up to 150℃ and one or two coordinated water molecules removed at 150~180℃.The octahedral structure is proposed fOr all the chelates, except Cu(II)-L2 and Ni(II)-L1 chelates which have square planar geometry, based on their electronic spectra

Uncatalyzed Condensation Reactions between Aromatic Aldehydes and Thiobarbituric Acid in Water

A series of 5-arylidene thiobarbituric acids were prepared from aromatic aldehydes and thiobarbituric acid in water without catalyst conditions in good yields. The structures were characterized by elemental analysis, IR and 1H NMR spectra.

Biochemical responses of freshwater fish Carassius auratus to polycyclic aromatic hydrocarbons and pesticides

The freshwater fish Carassius auratus was chosen as an experimental subject, and their hepatic biochemical responses to the medium-term exposure of Benzo（k）fluoranthene （BkF） alone and in combination with PCB 118 and dichlorodiphenyltrichloroethane （DDT） were investigated by measuring the reduced glutathione （GSH）, glutathione S-transferase （GST）, and thiobarbituric acid reactive substances （TBARS）, to assess sublethal effects. The hepatic GSH content was significantly inhibited by organic pollutants, alone and in mixtures, while the TBARS content was significantly induced after three days of exposure. Bell-shaped concentration-response charts of GST activities were obtained. Significant dose-response relationships were found for hepatic GSH and TBARS contents of all concentrations and for the GST activity, except at the highest concentration. The GSH content, GST activity, and TBARS content in Carassius auratus were confirmed as useful biomarkers of exposure to organic pollutions.

Transitional metal ions induced damage to biomolecules:role of ferryl and perferryl radicals

Objective:To investigate the effect of oxidized transitional metal（ferric and cupric） ions on the amino acids.Methods:25 mmol/L hydroxyproline and 25 mmol/L histidine were incubated with 50μL Fe3+ and Cu2+ ions at pH 7.4 and 37℃for 30 mins in separate test tubes.Then 500μL of 1% thiobarbituricacid（TBA） was added to the incubated amino acids followed by addition of 500μL of glacial acetic acid.The resultant mixture was vortexed and heated at 100℃for 30 min.Absorbance readings were noted after cooling to room temperature.The experiment was repeated in the presence of various reagents,like hydroxyl radical scavengers,antioxidant enzymes,and reducing agents and metal ion chelators.Results:The pink chromogen formed with the absorbance maxima at 524 nm,AND shifted to 560 nm in alkaline pH.The absorbance was expressed as TBAadduct in MDA units.The TBA-adduct decreased in the presence of reducing agents and metal ion chelators.Antioxidant enzymes and hydroxyl radical scavengers did not show any effect. Conclusion:Transitional metal ions in their oxidized state showed significant damage to amino acids,hydroxyproline and histidine.The results indicate the possible role played by high-valent oxo-iron species,ferryl and perferry radicals in damaging biomolecules.

Utilization of Virgin Coconut Meal (VCM) in the Production of Ready-to-Eat Indian Traditional Sweet Meat Using Response Surface Methodology

Virgin coconut meal (VCM) was used for the development of ready-to-eat Indian traditional sweet meat commonly known as “ladoo” both with and without sorbic acid (0.3%). The different ingredients were optimized following re-sponse surface methodology with three independent variables i.e. sugar, water and VCM and sensory attributes as responses. The changes in the quality of VCM ladoo packed in polypropylene (PP, 75 μ) and laminates of metalized polyester (MP, 75 μ) were monitored during storage to establish the shelf life under ambient temperature conditions (15?C - 34?C). Samples without added potassium sorbate spoiled within three weeks of storage due to mold growth and fermented odour. VCM ladoo containing sorbic acid did not support any microbial growth during storage up to 4 months, however, during storage samples packed in PP lost moisture and became hard and brittle, while those packed in MP remained soft. Peroxide and thiobarbituric acid values were higher in PP packed samples as compared to those packed in MP. Sorbic acid degraded during storage of ladoo and the rate of degradation was higher in PP packed ladoos than that in MP packed ones.

Possible Involvement of Reactive Oxygen Species Scavenging Enzymes in Desiccation Sensitivity of Antiaris toxicaria Seeds and Axes

The relationships among desiccation sensitivities of Antiaris toxicaria seeds and axes, changes in activities of superoxide dismutase （SOD）, ascorbate peroxidase （APX）, catalase （CAT）, glutathione reductase （GR） and dehydroascorbate reductase, （DHAR）, production rate of superoxide radical （.O2^-）, and the contents of hydrogen peroxide （H2O2） and thiobarbituric acid （TBA）-reactive substance were studied. Desiccation tolerance of seeds and axes decreased with dehydration. Desiccation tolerance of axes was higher than that of seeds, and that of epicotyls was higher than radicles. Activities of SOD, CAT and DHAR of seeds increased during the initial phase of dehydration, and then decreased with further dehydration, whereas activities of APX and GR decreased with dehydration. These five enzyme activities of axes, however, increased during the initial phase of dehydration, and then decreased with further dehydration. The rate of superoxide radical production, and the contents of H2O2 and TBA-reacUve products of seeds and axes gradually increased with dehydration. These results show that the A. toxicaria seed is a typical recalcitrant seed. Loss of desiccation tolerance in seeds and axes was correlated with the increase in .O2- production rate, content of H2O2 and TBA-reactive products, and the decline of antioxidant enzyme activities of seeds and axes.

Development of bis-thiobarbiturates as successful urease inhibitors and their molecular modeling studies

Bis-thiobarbiturate derivatives 1-15 have been synthesized, characterized by 1HNMR and El-MS and screened for urease inhibition. All compounds showed various degree of urease inhibitory activity with iC50 values ranging 7.45 ± 0.12 - 74.24 ± 0.81 μmol/L while the standard thiourea behaved normally （ICso = 21.10 ±0.12）. Compounds I （IC50= 7.45 ± 0.12 ]μmol/L）, 9 （IC50 =18,17 ± 1.03 bmol/L） and 13 （IC50= 8.61 ± 0.45 bmol/L） showed excellent urease inhibitory activity in the series. Molecular modeling studies were performed to understand the binding site with the bimetallic nickel center of the enzyme. Structure-activity relationship has also been established for these compounds. This study identified bis- thiobarbiturate as a novel class of urease inhibitors.

Neuroprotective role of antioxidant and pyranocarboxylic acid derivative against AlCl_(3) induced Alzheimer’s disease in rats

Objective:To assess potential of quercetin and etodolac to treat oxidative stress in neuronal death and inflammation in Alzheimer’s disease of AlCl3 induced rat models.All results of this AlCl_(3)model are compared with those obtained in controls.Methods:Wistar rats,housed in a controlled environment were treated with aluminum chloride(4.2 mg/kg of body weight,i.p.)for 28 d rather than oral to ensure neurotoxic concentration in hippocampus and hypothalamic region,part highly active in memory control and cognition,while control group was injected with saline.Estimation of thiobarbituric acid reactive substance,superoxide dismutase,reduced glutathione and acetylcholine levels gave estimation of neuronal damage.Low(20 mg/kg and 25 mg/kg)and high(40 mg/kg and 50 mg/kg)doses of quercetin and etodolac were administered to the test groups respectively.Histopathology study was conducted to perform relative study.Results:Co-administration of quercetin and etodolac either alone or in combination prevented the changes in biochemical markers of Alzheimer’s disease,but significant results(P<0.05)were seen when a combination of two was administered at low dose levels.Good correlation was developed between chemical estimations and histopathology study.Conclusions:Our findings suggest a combined role of anti-oxidant and cyclooxygenase inhibitor in protection of neural degeneration and inflammation due to oxidative stress.