Posted by admin on Nov 30, 2018 in |
Quantitative structure activity relationship is among the most widely used computational technology for analogue-based drug design. A molecular modelling approach using sulfadiazine- salicylaldehyde Schiff base analogue as anti-mycobacterial activity from recently reported literature were taken and was designed using MOE 2009.10. Sulfanilamide sulfa drugs have been shown to inhibit dihydropteroate synthetase. In order to develop a pharmacophoric model for this inhibition, quantitative structure-activity relationship (QSAR) for sulfa drugs active against DHPS have been studied. Multiple linear regression analysis was performed to derive quantitative structure activity relationship models which were further evaluated internally as well as externally for the prediction of activity. Accurate minimum inhibitory concentrations (µM) were collected for 19 analogs, and other parameters, such as partition coefficients, molar refractivity, dipole moment, electrostatic interactions, lowest unoccupied molecular orbital (LUMO), highest unoccupied molecular orbital (HOMO), topological polar surface area were calculated. A data set of 19 analogs, all having a common sulphadiazine moiety, provided a cross-validated correlation coefficient (r2) value of 0.5998 and root mean square error value of 0.3829....
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Posted by admin on Nov 30, 2018 in |
Diabetes mellitus relates a metabolic disorder of collective aetiology which is characterized by chronic hyperglycaemia caused due to disturbances of carbohydrate, lipid and protein metabolism due to impaired β cell function of pancreas or insulin resistance or both. Biguanides and Sulphonylureas are the most commonly prescribed drugs due to their efficacy and safety. A total of 60 patients were enclosed in the present study who met the inclusion criteria. They were divided into two groups based on their treatment plan-Group A and Group B. The Group B (P = 0.001) exhibited a significantly greater reduction in HbA1c as compared to Group A (P = 0.002). The reductions in FPG and PPG were also found to be significantly more in the Group B. In the present study, we observed that patients on Metformin-Teneligliptin exhibited better control over glycemic profile as well as lipid profile when compared to patients who are on Metformin-Glimepiride combination. Since, this study was conducted in less number of patients, to make consecutive remarks about the superiority...
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Posted by admin on Nov 30, 2018 in |
In the field of the preparation of chemotherapeutic agents with new mechanism distinct from currently approved drugs is important. However, the clinically effective approved small inhibitor molecule is still lacking. Previous reports indicated that 4-aryl-2-hydrazinothiazole derivatives provided a useful start point to develop HAT inhibitors (histone acetyltransferase). Consequently, preparation and biological evaluation of a focused library of 4-aryl-2-hydrazinothiazole based derivatives as useful as anti-cancer agents. Synthesis of 4-aryl-2-hydrazinothiazoles (1a-d), (2a-d), (3a-c), (4a-b), (5a-b), (6a-b) studied by either conventional method and free solvent microwave one-pot method, and the synthesized compounds were proved by spectroscopic methods (IR, 1HNMR, 13CNMR, GC-Ms, and elemental analysis). The activity against different cancer cell lines and the antimicrobial activities different organisms also studied, and all of the synthesized compounds were of high activity as an antibacterial for gram positive and gram negative; however, it showed also an antifungal activity were the most active compounds were 4a, 4b, 5b, 6a. It was found that all of the prepared thiazoles derivatives were active toward many cell lines (breast,...
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Posted by admin on Nov 30, 2018 in |
The elimination capacity of pristine powder activated charcoal PAC and powder activated charcoal modified with potassium permanganate MPAC to remove levocetirizine drug was investigated. The activated charcoal was impregnated with KMnO4 100 mg/L in order to improve the surface properties. The influence of concentration, time and pH on the adsorption of levocetirizine drug was conducted by means of UV-Vis spectroscopy. The experiments were carried out using two lines. Line 1; adsorption of the drug on pristine PAC and line 2; adsorption on MPAC. By batch experiments, the effect of levocetirizine concentrations of 25, 50, 75, and 100 mg/L, a reaction time of 15, 30, 45 and 60 min, and pH of 2, 4, 7 and 9 were investigated. The results showed that elimination capacity of both PAC and MPAC increased with increasing the drug concentration and time of contact and decreased with decreasing the pH. The elimination efficiency of MPAC found to be greater than that of...
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Posted by admin on Nov 30, 2018 in |
In response to several stressors such as intense light, fish elicit a generalized physiological stress response. Catla catla (61.3 ± 2.1 g) were exposed to five different light intensities of 983 ± 162 lx (L1), 1828 ± 324 lx (L2), 2676 ± 409 lx (L3), 3442 ± 648 lx (L4) and 114 ± 4 lx (Lc, control). Higher light intensities resulted in physiological stress, significantly (P<0.05) higher levels of heat shock protein-70 and heat shock protein-90 were found in both hepatopancreas and muscles of fish exposed at L4 treatment compared to the others to cope up with the stressor. A direct relationship was found between the light intensity and the serum glucose level. Significantly (P<0.05) higher glucose level was found in L4 exposed fish compared to the others. Fish at L4 had aggregated its pigments in the melanophores (punctate stage) to reflect intense light. This study could be useful in understanding the aspects of stress induced changes in fish skin melanophores. As a consequence of stress due to intense...
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