Posted by admin on Aug 1, 2014 in |
In this research, a new series of total twenty derivatives (39-58) of titled compound were synthesized with the help of substituted acetophenone which undergoes Aldol condensation reaction with dimethyformamidedimethylacetal (DMFDMA) to form corresponding unsaturated carbonyl compounds such as enaminones. The compound 2-thioxo-1,3-dihydropyridino[2,3-d] pyrimidin-4(1H)-one were obtained by reacting enaminones with 6-amino-2-thioxo-2, 3-dihydropyrimidin-4(1H)-one in the presence of dioxane. In this reaction, 6-amino-2-thioxo-2, 3-dihydropyrimidin-4(1H)-one acts as a nucleophilic reagent. Thus, the titled compounds were obtained by cyclizing an intermediate followed by desulphuration with the liberation of hydrogen sulphide gas in the presence of acetic acid. The homogeneity and purity of synthesized compound was ascertained by physical constant determination and chromatographic methods. The structure of the synthesized derivative was further confirmed by spectral (FTIR, NMR, MS) and elemental (C, H, N) analysis. The anticonvulsant activity of the compounds (39-58) was evaluated against Maximal Electroshock (MES)-induced seizures. The compounds, those found effective, were as well tested against subcutaneous pentylenetetrazole (scPTZ)-induced seizures model in mice. Using the rotorod procedure, the neurotoxicity was assessed. The results...
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Posted by admin on Aug 1, 2014 in |
Aceclofenac is new NSAID which demonstrates its anti-inflammatory and analgesic activity in a concentration of 1.5 %. Topical mode of administration help to avoid typical side effects associated with oral administration of NSAIDS such as irritation and ulceration to gastric mucosa. Hence, an attempt has been made to prepare topical formulations using various dermatological bases and to evaluate release properties and improved stability throughout its shelf life. Cream, gel and emulgel topical formulations were formulated and characterized for its physicochemical parameters such as pH, spread ability, rheological properties and occlusivity. The in-vitro permeation potential of Aceclofenac was performed through Dow Corning 7-4107 silicone elastomer membrane using Franz type diffusion cell. The in-vitro permeation rate of drug from silicone cream base was significantly higher compared to other vehicles. The in-vivo animal study was performed on croton oil induced ear edema model. Developed Aceclofenac cream formulation showed 66.67% inhibition of ear edema which was significantly higher than other formulation. The stability study of Aceclofenac formulations was performed at 25°C/60 % RH,...
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Posted by admin on Aug 1, 2014 in |
Man, the superior most of all species has always been remaining in a search of One Prime Goal: “The perfect health”. From Vedic era to space age, all the researches have been directed by the eminent scholars to achieve the same. Vrana (wound) is one of the critical conditions which have been managed by human being from starting of civilization. The present work is a substantial step for wound healing. Ingudi {Balanites aegyptiaca (Linn.) Delile} is well known plant used for wound healing with their specific property like laghu, snigdha guna, tikta, katu Rasa, katu Vipaka, ushna Virya and krimighna Prabhava since ancient era. Not only in Ayurvedic literature, in Sanskrit literature also have we found its description for wound healing (Abhigyan shakuntalum...
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Posted by admin on Aug 1, 2014 in |
The uses of plant-based products for disease prevention and treatment become increasingly popular in many societies. Plants are considered one of the major sources for many bioactive groups such as alkaloids. The purpose of this study was to determine the rate of alkaloids and investigate antibacterial activity of alkaloid fraction of seeds and leaves from plant, genus Swietenia of S. macrophylla (Familay: Maliaceae) against four pathogenic bacteria namely; Gram-positive: Staphylococcus aureus ATCC1026 and Gram-negative: Escherichia coli ATCC10536, Pseudomonas aeruginosa ATCC15442, and Salmonella typhimurium ATCC14038 based on inhibition zones. For the antibacterial bioassay, two concentrations, 50 and 100 mg/mL of seeds and leaves extracts were prepared and tested by disc diffusion method. The obtained results showed that the plant parts contain various levels of alkaloids, and with appreciable level of antibacterial activity against all tested microorganisms. The seeds extract showed high activity at a concentration of 100 mg/mL compared with leaves at the same concentration, especially against Gram-positive strain. The inhibition zones ranged from 3 to 21 mm for all...
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Posted by admin on Aug 1, 2014 in |
Cancer is one of the major threats to human health that cause considerable suffering and economic loss worldwide. The search for natural compounds which prevent cancer has upsurge with the mounting evidence that many types of cancer are caused or triggered by factors relating to our lifestyle. Chemopreventive agents include all those agents which can either prevent cancer or slow down the growth of malignant lesions. The present experiment was designed to explore the chemoprotective and antioxidative potential of Flaxseed oil (FSO) on 7, 12-dimethylbenz(a)anthracene (100 μg/100 μl of acetone) and croton oil (1% in acetone/three times a week) induced skin carcinogenesis in mammals. FSO administration to mice, by oral gavage at a dose of 50µl/animal/day for 17 weeks at peri-post initiation stage (i.e. started from 7 days before the experiment & continued till completion of experiment), reduced the tumor burden, tumor multiplicity, tumor yield, cumulative number of papillomas and percent tumor incidence while increased the average latent period when compared to control group. The lipid per oxidation levels...
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