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 |
The motivation behind composing this review on floating drug delivery systems (FDDS) was to incorporate the ongoing research article with a unique spotlight on the key system of floatation to accomplish gastric maintenance. The ongoing advancements of FDDS, including the physiological and formulation factors influencing gastric maintenance, ways to deal with configuration single-unit, and numerous unit of floating drug delivery systems, and their grouping and formulations perspectives are canvassed in detail. This review has a special focus on the principal mechanism of floatation to achieve gastric retention. Conventional oral dosage forms have short residence times & unpredictable gastric emptying time. The idea of gastric retention comes from the need to localize drugs at a specific region of the gastrointestinal tract (GIT), such as the stomach in the body. Many drugs get absorbed only in the upper intestinal tract, designing such molecules as once-daily formulations are exclusive for these molecules. Thus, gastro retention could help to provide greater availability of new products and consequently improved therapeutic activity and substantial benefits...
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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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