Posted by admin on Feb 28, 2021 in |
Background: Epilepsy is a chronic disorder that causes unprovoked, recurrent seizures like a sudden rush of electrical activity in the brain. Neuronal hyperexcitability in epilepsy is due to an imbalance between glutamate-mediated excitation and GABA-mediated inhibition. Aim: This prompted us to design newer CSF1R inhibitors as efficient therapeutic drugs for the treatment of epilepsy. Materials and Methods: Based on the common pharmacophoric features for the inhibition of CSF1R inhibitors, a series of leads were designed using computational methods. A virtual library consisting of newly designed 60 molecules as CSF¬1R inhibitors were constructed .Based on these facts, a virtual library has been generated with 60 newly designed ligands containing imidazole, benzo pyrrole, quinoline, oaxzole, quinoxaline, benzimidazole, heterocyclic nucleus as CSF1R inhibitors (60). The binding mechanism of newly designed ligands with target enzymes CSF1R inhibitors was studied using Auto dock tools 1.5.6. Conclusion: The designed compounds were subjected and filtered by applying ADMET properties. In comparison with docking scores of standard antiepileptic drugs vigabatrin (GABA-2.14, CSF1R-1, 31) and sodium valproate (GABA-3.19,...
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Posted by admin on Feb 28, 2021 in |
Tuberculosis holds one of the top places on the list of the main cause of death in India. At times, the patients fail to respond to treatment with anti-Tb drugs, drug resistance being one of the reasons. The increasing incidence of MDR and XDR-TB highlights the urgent need to search for newer anti-Tb drugs. For last many years, plants have beneficial activity in a different types of diseases producing in human beings. As per WHO calculation about 80% of the world’s inhabitants problem should treat by medicinal herbal drugs for their primary health care. So, the present aim to carry out the evaluation of the anti-mycobacterial activity of selected eleven medicinal plants. Three different extracts were prepared and evaluated for their antimycobacterial activity against Mycobacterium smegmatis using MTT and Microplate Resazurin assay. Isoniazid was used as a standard drug. The percentage for anti-mycobacterial smegmatis activity among tested eleven medicinal plants, an aqueous extract of Cocculus hirsutus and Leptedinia reticulata shows potent antimycobacterial activity. Thus, its result supports the uses...
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Posted by admin on Feb 28, 2021 in |
Dabigatran mesylate is a novel oral anticoagulant that works by blocking the clotting protein thrombin. The present work describes the separation and quantification of potential impurities in a single HPLC method, which are generated from raw materials to API synthesis. This method is capable of separating and quantifying the fourteen impurities, produced from the intermediate stages to final drug substance stage of dabigatran within 40 min of run time. Column: Poroshell 120, EC C-18, 150 mm × 4.6 mm, 2.7 µ; Buffer: 2.04 g of Potassium dihydrogen phosphate in a beaker, add 1500 mL of water and dissolve, to this add 1.5 ml Triethylamine (TEA) and 1 ml of Phosphoric acid; Diluent: water and acetonitrile in the ratio 20:80% v/v; The flow rate: 0.7 mL/min; Column temperature: 40 °C. Wavelength: 230 nm; The drug substance was subjected to stress studies such as hydrolysis, oxidation and thermal degradation and considerable degradation was observed in acidic hydrolysis and oxidative stress conditions. The formed degradation products were well-resolved from the dabigatran drug...
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Posted by admin on Feb 28, 2021 in |
Benzofuranones and nitrogen mustards have been reported as highly potential alkylating agents; with this evidence, the synthesis of some benzofuranones fused with nitrogen mustards was planned and was subjected to in-vitro cytotoxic studies. Substituted benzofuranones were synthesized by condensation of 2-hydroxy benzaldehydes and substituted 2-hydroxy acetophenones and further fused with nitrogen mustards gave high yields of target compounds 2 – (2 – (2 – (Bis (2 -chloroethyl) amino) ethoxy) benzylidene) benzofuran-3(2H)-one derivative. The derivatives synthesized had various halo substitutions such as chloro, bromo, fluro and methyl chloro derivatives. These synthesized compounds were characterized by FTIR, 1H NMR and LCMS spectral studies. Further, the synthesized compounds were subjected to 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide assay on human lung carcinoma cells, A-549 and breast cancer cells, MCF-7 for its in-vitro cytotoxic activity. All the synthesized compounds showed promising cytotoxic activity in which AN– O – 04, (Z) – 2 – (2 – (2 – (bis (2 -chloroethyl) amino) ethoxy) benzylidene) -5 – chloro – 6-methylbenzofuran-3(2H)-oneshowed minimum CTC-50 of 119.32 ± 8.98...
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Posted by admin on Feb 28, 2021 in |
The effect of constant lighting on the level of some hematological parameters and their daily dynamics was studied in male Wistar rats at the age of 6 months. It was found that staying in constant light for 3 weeks leads to a rise in hematocrit level, mainly due to an increase in the number of red blood cells, while a decrease in the oxygen-transporting properties of these cells is noted. An analysis of the diurnal dynamics of the studied parameters, it was found that the keeping of animals under constant illumination destroys the circadian rhythms of HGB, MCV, RDWc, PCT, MPV, PDWc, and MCHC. The destruction of the circadian rhythms found in control is most likely due to both a decrease in the level of melatonin in constant light and a violation of its own circadian rhythm in the absence of a pacemaker, which role is played by the alternation of light and...
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