Posted by admin on Feb 26, 2015 in |
A series of novel 1-(2-(4-fluorobenzylthio)pyrimidin-4-yl-amino)-4-(substituted phenyl)azetidin-2-one analogues (3a-e) were synthesized starting from 2-thiouracil. Reaction of 2-thiouracil with 4-fluorobenzylchloride gave 2-(4-fluorobenzylthio) pyrimidin-4(3H)-one which on chlorination with POCl3 yielded 2-(4-fluorobenzylthio)-4-chloropyrimidine. Further reaction of compound 2-(4-fluorobenzylthio)-4-chloropyrimidine with hydrazine hydrate generated the key intermediate 1-(2-(4-fluorobenzylthio)pyrimidin-4-yl)hydrazine (1). Reaction of compound 1 with appropriate substituted aromatic aldehydes furnished 2-(substituted benzylidene)-1-(2-(4-fluorobenzylthio) pyrimidin-4-yl)hydrazine (2a-e), which on further cyclisation with acetyl chloride in dry benzene furnished 1-(2-(4-fluorobenzylthio)pyrimidin-4-yl-amino)-4-(substituted phenyl) azetidin-2-one analogues (3a-e). Structural assignments of the synthesized compounds were based on their IR, 1H NMR, Mass and analytical data. All the synthesized compounds 3a-e were screened for their preliminary antimicrobial properties. Some of the compounds exhibited promising antimicrobial...
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Posted by admin on Feb 26, 2015 in |
Antihypertensive properties of plant can be evaluated by in vitro method on inhibition of Angiotensin Converting Enzyme (ACE) activity. In this research, we investigate the inhibitory effect of several common edible plants on blocking ACE activity. ACE activity was evaluated by using N-hippuryl-L-histidyl-L-leucine (HHL) as substrate and the inhibitory effect of extracts were determined based on the level of hippuric acid by measuring its absorbance using spectrophotometer. Gelatin-salt block test for detection of tannins was carried out prior to the enzymatic assay. Among the extracts tested, Peperomia pellucida L. showed strong inhibitory activity with IC50 value of 7.17μg/mL, followed by Nasturtium officinale and Sesamum indicum L. with IC50 values of 15.44 and 30.16μg/mL, respectively. Furthermore, Peperomia pellucida was the most potent inhibitor of ACE activity in vitro with IC50 value of 7.17 µg/ml, which was comparable to that of captopril (13.68 µg/ml), a potent ACE inhibitor. This study shows that these plants may develop as antihypertensive...
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Posted by admin on Feb 26, 2015 in |
Peptic ulcers is one of the major gastrointestinal disorder in human being that generally associated with the infection of Helicobacter pylori, a gram-negative microaerophilic bacterium in stomach. It is also linked to the development of the stomach cancer. The aim of this study was to investigate the in vivo properties of the sub-unit pili proteins with molecular weight of about 49,6 kDa in mice. The bacterium was firstly cultured on the plate of TSA-B (Trypticase Soy Agar with 5% Sheep Blood) to prepare the protein of interes using bacterial cutter and SDS-PAGE. The purified protein was used for a vaccine emulsified with commercial cholera toxin and give orally. The immunized mice showed a significant protection against challenge with live H. pylori cells. In contrast, animals that received the 49, 6 kDa protein without adjuvant as well as the negative control with PBS failed to inhibit adherence of the bacteria, as indicated by a severe damages of gastric tissues. This study has indicated that the sub-unit pili proteins trigered the...
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Posted by admin on Feb 26, 2015 in |
To develop and validate simple and precise methods RP – HPLC (Method A) and Dual wavelength method (Method B) for simultaneous estimation of Simvastatin (SIM) and Sitagliptin (SITA) in combined dosage form. Methods used are Method A, the chromatographic separation was achieved by using mobile phase acetonitrile: methanol: water (50:30:20), a C18 column. The mobile phase was pumped at a flow rate 1 ml /min and the eluents were monitored at 250 nm. Method B, two wavelengths were selected for each drug in such a way that the difference in absorbance is zero for the second drug. At wavelengths 225 and 248 nm SITA has equal absorbance values, therefore, these two wavelengths have been used to determine SIM, on similar basis 254 and 274 nm were selected to determine SITA in the combined...
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Posted by admin on Feb 26, 2015 in |
Malathion is a widely used organophosphorous pesticide that a large number of populations are undesirably exposing themselves to severe health risk due to taking up the contaminated foods, water and vegetables containing malathion. The present study was carried out through histopathologic test to evaluate the extent of damage caused by malathion in the liver and kidney tissues of mice. Twenty five adult female albino mice were used and dispense mainly into two groups as control group and treatment group. The mice of control group were feed with poultry food without any ingredient of malathion. Each of the treatment groups (group1, group 2, group 3 and group 4, containing five animals in each group) were supplied everyday with the same type of food containing the following amounts of malathion as 65mg, 13mg, 2.6mg, and 0.52mg per 50gm (10gm food/mouse) of food, respectively. After fifteen days the animals of both groups were sacrificed and the organs of sacrificed animal were subjected to histopathological examination and then visualized under light microscope. Results...
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