SYNTHESIS AND DOCKING STUDIES OF 2-(NITROOXY)-ETHYL-2-(SUBSTITUTED-2,5-DIPHENYL-OXAZOLE)-ACETATE AS ANTI-INFLAMMATORY AGENTS WITH ANALGESIC AND NITRIC OXIDE RELEASING PROPERTIES

Objective: The objective of the reported study was to develop new chemical entities as potential anti-inflammatory agents with analgesic and nitric oxide releasing properties.Methods: The compounds were designed with the help of docking studies. In the synthetic study the target compounds were obtained by reacting 2-(substituted-2,5-diphenyl-oxazole)-acetic acid (2a-2v) with nitro-oxy ethyl bromide in the presence of dimethyl formamide and potassium carbonate to give 2-(nitrooxy) ethyl 2-(substituted-2,5-diphenyl-oxazole) acetate derivatives (3a-3v). The synthesized derivatives were characterized with the help of different analytical techniques and further evaluated for anti-inflammatory, analgesic and nitric oxide releasing activity.Results: With the help of docking study it was proven that compounds 3a, 3c, 3g, 3l and 3r showed significant G-score. In the anti-inflammatory and analgesic study also, compounds 3a, 3c, 3g, 3l and 3r exhibited promising activity. All the synthesized compounds exhibited significant nitric oxide releasing properties both in-vitro and in-vivo. Conclusion: Compounds 3a, 3c, 3g, 3l and 3r exhibited prominent anti-inflammatory and analgesic activity.Â

Optimization of process variables for phyllanthin extraction from Phyllanthus amarus leaves by supercritical fluid using a Box-Behnken experimental design followed by HPLC identification

The response surface methodology using the Box-Behnken design was established to describe supercritical carbon dioxide assisted extraction of phyllanthin from Phyllanthus amarus Schum and Thonn leaves prior to HPLC analysis. The effects of extraction pressure, temperature, modifier concentration and extraction time on the yield of phyllanthin were investigated. By solving the regression equation, the optimum conditions were as follows: extraction pressure 23.2 MPa, temperature 40 °C, methanol as modifier at a concentration 10 % and time 90 min. Under these conditions, the phyllanthin yield was 12.83 ± 0.28 mg g-1, which was in good agreement with the predicted values. Modifier concentration and extraction time showed a significant effect on the phyllanthin yield

SYNTHESIS AND DOCKING STUDIES OF 2-(NITROOXY) ETHYL-4-(2-(SUBSTITUTED PHENYL)-4-(SUBSTITUTE DPHENYL)-1H-IMIDAZOL-1-YL) BENZOATE AS ANTI-INFLAMMATORY, ANALGESIC AND NITRIC OXIDE RELEASING AGENTS

Objective: The objective of the present study was to develop potent and non toxic Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) by using heterocyclic nuclei and having Nitric Oxide releasing group.Methods: The compounds were designed with the help of docking studies. In the synthetic study, the target compounds were obtained by reacting substituted diphenyl imidazole benzoic acid (2a-2x) with nitro-oxy alkyl bromide in the presence of dimethyl formamide and potassium carbonate to give substituted 2,4-diphenyl nitric oxide releasing imidazole derivatives (3a-3x). The synthesized compounds were characterized with the help of different analytical studies and further evaluated for anti-inflammatory, analgesic and nitric oxide releasing activity.Results: In the docking study compounds 3a, 3b, 3c, 3e, 3r and 3s showed significant G-score. In the anti-inflammatory and analgesic study compounds 3a, 3b, 3c, 3e, 3r and 3s exhibited promising activity. All the synthesized compounds exhibited significant nitric oxide releasing properties both in-vitro and in-vivo. Conclusion: Compounds 3a, 3b, 3c, 3e, 3r and 3s exhibited prominent anti-inflammatory and analgesic activity.Â

Densitometric Determination of Risedronate Sodium in Tablets

An HPTLC method for analysis of risedronate sodium in bulk and pharmaceutical formulation has been established and validated. The analyte was separated on aluminium plates precoated with silica gel 60 F254 . The mobile phase was water-acetontrile-ammonia solution 9.3:0.40:0.3 (v/v). Quantification was done by densitometric scanning at 262 nm. Response was a linear function of risedronate asdium concentration in the range of 5 to 25 μg/mL. The limit of detection and quantification for risedronate sodium were 0.86 and 3.03 μg/mL respectively. Average recovery of risedronate sodium was 99.31, which shows that the method was free from interference from excipients present in the formulation. The established method enabled accurate, precise, and rapid analysis of risedronate sodium in bulk as well as pharmaceutical formulation.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Analgesic and anti-inflammatory activities of saponified fraction from Annona reticulata L. Bark

The saponified petroleum ether extract (SPE) of the Annona reticulata L. bark were studied for fatty acid composition by GC-MS analysis. Six fatty acids amounting 86.68% of the total contents were identified. The composition of saturated and unsaturated fatty acid was 22.10 % and 64.58 %, respectively. SPE at the doses of 12.5, 25 and 50 mg/kg body weight showed significant central as well as peripheral analgesic, along with anti-inflammatory activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Densitometric Determination of Risedronate Sodium in Tablets

An HPTLC method for analysis of risedronate sodium in bulk and pharmaceutical formulation has been established and validated. The analyte was separated on aluminium plates precoated with silica gel 60 F254 . The mobile phase was water-acetontrile-ammonia solution 9.3:0.40:0.3 (v/v). Quantification was done by densitometric scanning at 262 nm. Response was a linear function of risedronate asdium concentration in the range of 5 to 25 μg/mL. The limit of detection and quantification for risedronate sodium were 0.86 and 3.03 μg/mL respectively. Average recovery of risedronate sodium was 99.31, which shows that the method was free from interference from excipients present in the formulation. The established method enabled accurate, precise, and rapid analysis of risedronate sodium in bulk as well as pharmaceutical formulation.Colegio de Farmacéuticos de la Provincia de Buenos Aire

An alum [KAl (SO4)2.12H2O] catalyzed microwave assisted multicomponent synthesis of bioactive functionalized benzylpyrazolyl coumarin and quinolinone derivatives in PEG

An efficient and environmentally benign method has been developed for the synthesis of benzylpyrazolyl coumarin and quinolinone derivatives, hydroxy coumarin derivatives using Alum [KAl (SO4)2.12H2O] catalyst and Polyethylene glycol as green solvent under microwave condition. Keywords: Knoevenagel, Michael addition reaction, coumarins, quinolinones, alum, polyethylene glycol, multicomponent microwave irradiation method

Green synthesis and anxiolytic activity of some new dibenz-[1,4] diazepine-1-one analogues

AbstractA facile, green approach for the synthesis of some new dibenz[1,4]-diazepine-1-one by a three component reaction of Diamine, 1,3 diketone and aromatic aldehyde using oxalic acid as catalyst in water is described. The products are formed in good yields (92–94%). Newly synthesized dibenz [1,4]-diazepine-1-one analogues were evaluated for the anxiolytic activity by the elevated plus maze method. From the activity data it is observed that compounds, 4g, 4h and 4k show promising anxiolytic activity

Stability-indicating HPLC determination of pramipexole dihydrochloride in bulk drug and pharmaceutical dosage form

A novel stability-indicating high-performance liquid chromatographic assay method was developed and validated for quantitative determination of pramipexole dihydrochloride in bulk drugs and in pharmaceutical dosage form in the presence of degradation products. An isocratic, reversed phase HPLC method was developed to separate the drug from the degradation products, using an Ace5-C18 (250×4.6 mm, 5 µm) advance chromatography column, and 10 mmol L-1 ammonium acetate and acetonitrile (75:25 v/v) as a mobile phase. The detection was carried out at a wavelength of 260 nm. The pramipexole was subjected to stress conditions of hydrolysis (acid, base), oxidation, photolysis and thermal degradation. Degradation was observed for pramipexole in base, in acid and in 30% H2O2. The drug was found to be stable in the other stress conditions attempted. The degradation products were well resolved from the main peak. The percentage recovery of pramipexole was from (99.87 to 99.98%) in the pharmaceutical dosage form. The developed method was validated with respect to linearity, accuracy (recovery), precision, system suitability, specificity and robustness. The forced degradation studies prove the stability indicating power of the method

TiCl₄ Promoted synthesis of benzimidazole derivatives

349-351Differently substituted benzimidazoles have been synthesised in very good yields in solvent-free conditions from o-phenylenediamine and aldehydes in the presence of TiCl₄ as a catalyst. The method is applicable to aromatic, unsaturated and aliphatic aldehydes and to substituted o-phenylenediamines without significant differences