Posted by admin on Jan 31, 2017 in |
In the present study 17 novel benzaldehyde thiosemicarbazone derivatives were synthesised using 2-methyl-3-thiosemicarbazide as the main reactant and different aromatic aldehydes. Reactions were monitored using thin layer chromatography technique and the newly synthesised derivatives were characterized by Elemental analysis, ATR and 1HNMR techniques. For antibacterial activity four bacterial strains were selected namely Bacillus subtilis (gram +ve), Staphylococcus aureus (gram +ve), Escherichia coli (gram –ve), and Pseudomonas aeruginosa (gram -ve).Candida albicans was used to ascertain the antifungal activity of compounds. Antimicrobial assay was performed using nutrient agar media for the bacterial strains and Sabouraud agar for the fungus, zone of inhibition of all the compounds which could inhibit visible growth after incubation were calculated. Four different dilutions of the test compounds were taken and compared against ciprofloxacin and fluconazole as the standard drugs. Antimicrobial assay was performed in duplicate. The test compounds were active against both gram negative as well as gram positive bacteria. Considerable anti-fungal was shown by the compounds. Antioxidant assay was performed using 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) or ABTS...
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Posted by admin on Jan 31, 2017 in |
Recent decades have experienced a sharp increase in the incidence and prevalence of diabetes mellitus. The major therapeutic approach is to diabetes is to reduce gastrointestinal glucose production and absorption through the inhibition of carbohydrate digesting enzymes such as α-amylase and α-glucosidase. The agonists of PPAR γ is of great interest to the pharmaceutical industry since they regulate the expression of genes Associated with diseases like cancer, diabetes, atherosclerosis and obesity The aim of the current study was to synthesize newer PPAR γ agonists with alleged antidiabetic properties for α-amylase and α-glucosidase inhibitory activities. Newer PPAR γ agonist ligands containing three parts acidic head, a linker, and a hydrophobic tail as Pharmacophore features were designed. Four different compounds containing thiazole as heterocyclic nucleus have been synthesised and characterised by analytical methods like IR, NMR, spectral data. All the synthesised molecules were Optimizied using Lipinksi’s rule of five and subjected to docking studies using ARGUS LAB 4.0. Docking studies showed the important interactions of lead molecules posses with some of...
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Posted by admin on Jan 31, 2017 in |
Due to your efforts diligent on quinoline nucleus new series containing pyrimido [4, 5-b] quinoline were synthesized via starting with the strategic 2-aminoquinoline-3-carbonitrile (2) intermediates to afford various pyrimido [4, 5-b] quinoline via cyclization with different reagents to get compounds 3-24. Compounds 3, 6, 9a, 9b, 12, 15, 16a, 16b, 17, 21 and 24 were tested for in vitro antitumor activity against human breast carcinoma (MCF-7) cell line, We found what we were hoping for where compound 6 was found the most active member (IC50= 48.54 μM) than the Doxorubicin as a reference drug with (IC50= 71.80 μM). To understand the interaction of binding sites with the target protein receptor, the docking study was performed using topoisomerase II. The results of in vitro cancer activity and docking study revealed that the synthesized compounds have potential cancer activity and can be further optimized and developed as a lead...
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Posted by admin on Dec 31, 2016 in |
Proniosomes based drug delivery systems have potential as a significant drug carrier in a variety of therapeutic applications. The objective of the present study was to investigate in vitro sonophoretic transdermal delivery of Losartan Potassium (LP) across albino rat skin using proniosomal gel and its comparison with aquasonic gel. Proniosomes of LP were fabricated with L-a-lecithin (egg yolk), cholesterol and a non-ionic surfactant and confirmed using optical microscopy. Permeation experiments were performed using modified Franz Diffusion Cell along with ultrasound treatment (Frequency-1MHz; Intensity- 2.5 W/cm2; Duration of application- 30 min; Mode of application – Continuous and Pulsed). An in vitro skin permeation of LP with aquasonic gel was found superior than proniosomal gel using sonophoretic delivery. Using proniosomal gel, when ultrasound was applied in pulsed mode, LP transdermal flux and enhancement factor were 60.88 ± 6.2 μg/cm2/h and 5.31, respectively, 115.41 ± 5.01 μg/cm2/h and 10.07 those achieved using aquasonic ultrasound gel, respectively. Similar results were observed (better flux with aquasonic gel than proniosomal gel) using continuous mode of...
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Posted by admin on Dec 31, 2016 in |
Anti-diabetic activity of hydro-alcoholic extract of Chrysophyllum cainito frutis (CCE) was investigated against experimentally induced diabetics in rats using alloxan and streptozotocin (STZ). Acute toxicity study was performed and hydro-alcoholic extract of CCE was found to be safe at a dose of 2000 mg/kg bodyweight. Two doses 200 mg/kg and 400 mg/kg b.w p.o. of the CCE were subjected for the evaluation of anti-diabetic activity against the diabetic induced by alloxan (100 mg/kg, i.p) and STZ (50 mg/kg, i.p) in rats. Glibenclamide (5 mg/kg p.o) was served as standard in both the models. Fasting blood glucose, serum total cholesterol, serum triglycerides, lipid profile (HDL and LDL) and histopathology were evaluated in the study. Both the lower (200 mg/kg) and higher dose (400 mg/kg) of CCE showed a dose dependent significant decrease in blood glucose level, triglyceride, cholesterol levels and LDL and an increase in HDL in the treated diabetic rats when compared with diabetic control. Histopathology of pancreas showed regeneration of β-cells in extract treated diabetic rats. The results...
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