Posted by admin on Jun 30, 2022 in |
Furan and Azetidinone have been reported to possess various therapeutic activities, including anti-microbial and anti-cancer activity. Increasing drug resistance and high toxicity to the existing drugs have dictated the need to develop novel, effective agents with different scaffolds. With the perspective of identifying novel anti-cancer molecules, an approach was made to hybridize the different heterocyclic moieties. Thirtynovel Furan-Azetidinone hybrids were subjected to in-silico molecular docking studies to determine the novel molecules’ affinity for the anti-cancer targets. The four most promising derivatives were selected and synthesized based on docking scores. Condensation of ethyl cyanoacetate and o-toluidine at 160-1900C yielded 2-cyano-N-2(methylphenyl) acetamide (1). The reaction between (1) and benzoin yielded 2-amino-N-(2-methylphenyl) 4, 5-diphenylfuran-3- carboxamide (2). A series of Schiff bases ARJJ03 (1-2), were synthesized from (2) by refluxing it with various substituted aromatic aldehydes in ethanol using concentrated sulphuric acid as the catalyst. The title compounds ARJJ04 (1-2) were obtained by the cyclization of ARJJ03 (1-2) with Chloroacetyl chloride in 1, 4-dioxane in the presence of triethylamine. The synthesized derivatives were...
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Posted by admin on Jun 30, 2022 in |
Candesartan cilexetil is widely used for the treatment of hypertension. Candesartan cilexetil is a pro-drug administered orally, rapidly converted to its active metabolite candesartan during absorption in the gastrointestinal tract. Candesartan cilexetil is a BCS II drug that is practically insoluble in the water of 0.00771 mg/ml & it has a low dissolution rate, hence; to improve dissolution rate & bioavailability, solid dispersion of Candesartan cilexetil were prepared by kneading method, solvent evaporation method & Microwave method in 1:0.5, 1:1 & 1:1.5 ratios of Candesartan cilexetil and hydroxy propyl beta-cyclodextrin /PVP K 30. Further, the SDs were filled into empty hard gelatin capsules with excipients like starch (8%), lactose, talc & Aerosil by manual capsule filling method. The formulated solid dispersions were evaluated for drug content and in-vitro dissolution studies. Accelerated stability studies was conducted for the optimized SD formulations, the optimized drug & carrier SD were confirmed & characterized by FT-IR. The drug content of the prepared Candesartan cilexetil SD formulations was found to be range from 94.35±0.95%...
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Posted by admin on Jun 30, 2022 in |
Ornamental plants (OPs) are used for intensifying, glorifying surroundings, adding a positive attitude towards life, enhancing estate value, and developing a feeling of well-being and happiness. This research aimed to record the ornamental plants and ethnomedicinal document usage of the plants by the local people of the Rewari district of Haryana State. The data was collected through field surveys and in-depth interviews organized with 219 local informants from the region during 2019-21. A total of 80 different locations were visited during the study. 91 OPs belonging to 83 genera and 42 families were identified and documented from the Rewari district. The documented plants showed a diversity of habit ranging from herbs (43.96%), trees (24.18%), shrubs (24.18%), twines (3.30%), and climbers (3.30%) and creepers (1.10%). The majority of ornamental plants were utilized as garden plants (25.50%) followed by pot (25.19%), bouquet/ cut flower/ cut foliose (11.41%), avenue (9.44%) road dividers (7.87%), religious and cultural (7.87%). Families Leguminosae (11.95%) and Asteraceae (7.60%) were the dominant families. Maximum no. of ethnomedicinal uses...
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Posted by admin on Jun 30, 2022 in |
Objective: The present work aimed to prepare flurbiprofen tablets using different concentrations of super disintegrants like croscarmellose sodium, sodium starch glycolate cross povidone sublimating agent thymol. Methods: The tablets were prepared by direct compression and sublimation technique using different concentrations of super disintegrants. The prepared tablets were evaluated for different parameters like hardness, friability, weight variation, thickness, content uniformity, wetting time, disintegration time, and dissolution study. Morphology of pure drug and optimized formulation were revealed by using SEM. Results: All the formulations prepared with the highest concentration of super disintegrant showed the highest drug release. Formulations from F11 to F13 were prepared with the sublimation technique. F11 formulation showed the highest drug release because of its porous nature, which resulted from the sublimation technique. Conclusion: The optimized formulation of the sublimation method (F11) was porous in nature. In-vitro drug release of all formulations prepared with the highest concentration of super disintegrant showed higher drug release than lower concentrations. The formulations prepared by the sublimation technique showed good drug release...
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Posted by admin on Jun 30, 2022 in |
This current investigation was designed to assess in-vitro the ability of the extract to prevent free radical-induced oxidative cell damages. Fibroblasts were exposed to hydrogen peroxide and treated with gradual concentrations of ethanol and dichloromethane fruits pulp extracts from Adansonia digitata and Ziziphus mauritiana. The cell viability was measured after 24h of treatment by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium (MTT) assay. Moreover, the capacity of extracts to scavenge free radicals was evaluated by using the DPPH and ABTS models. The polyphenol contents of extracts were also quantified by spectrophotometry. All extracts in a concentration between 100 and 400 µg/mL didn’t exhibit any cytotoxic effects on fibroblasts compared to the vehicle (p >0.05). However, extracts showed interesting cytoprotective activity against the hydrogen peroxide-induced oxidative cell damage. The cytotoxic effects of the hydrogen peroxide were completely suppressed by adding the extracts of A. digitata. The ethanol extract of A. digitatas showed the best free radical quenching activities on DPPH radical (IC50 = 28.78 ± 4.97 µg/mL) and ABTS radical (IC50 =25.29 ±...
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