Posted by admin on Jan 31, 2022 in |
Amantadine hydrochloride (1) is an antiviral drug currently used to treat certain influenza infections (type A). It is also used as an anti-dyskinetic agent to treat Parkinson’s disease. Several methods for the preparation of amantadine hydrochloride (1) were reported, these procedures started from adamantane (2), using procedure four reaction steps to obtain amantadine hydrochloride with an overall yield of 46-58%. In this article, we present a convenient two-step procedure for the synthesis of 1 from 1-bromoadamantane (3) and acetylamide in the presence of sulfuric acid via N-(1-adamantyl) acetamide (4) in one-pot with an overall yield of 74%. The procedure was also optimized to reduce the use of toxic reagents and solvents to make it to safer and more environmentally friendly. The procedure can be considered as more suitable for large-scale production of amantadine hydrochloride. The structure of the obtained amantadine hydrochloride was confirmed by MS, IR, 1H-NMR and...
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Posted by admin on Jan 31, 2022 in |
Paramphistomiasis is the major problems in the yield of goat and human health. This disease causes loss of life of goat, reduce meat and milk production. The medicinal plant Capparis decidua has been used in the treatment of asthma, cough and inflammation. This plant also shows anthelmintic activity. Live amphistome Gastrothylax crumenifer were collected from the rumen of the freshly slaughtered goats at local meat market of Chittorgarh. Amphistomes Gastrothylax crumenifer was maintained in 0.9% physiological saline and divided into four groups; first group used for identification, second group as control or untreated, third group for treatment with Capparis decidua and fourth group for treatment with synthetic drug albendazole. The histological study of treated and control tegument of Gastrothylax crumenifer was observed by light microscopy. Extract of Capparis decidua caused many topographical changes in Gastrothylax crumenifer like discontinuation, distortion, peeling and damaging cells, vacuolization and deformation in the muscles fiber, found blebblings in tegument. Albendazole is less effective than alcoholic extract of Capparis decidua (Kair). This study suggests the...
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Posted by admin on Jan 31, 2022 in |
Independent studies have shown that chalcones and 123 triazole exhibited cytotoxic effects on human cancer cell lines. In the present study, we prepared a series of novel 1,2,3-triazole-chalcone hybrid compounds and evaluated the cytotoxic effect and probable mode of action in HT29 colon cancer cell line. Among the 10 evaluated compounds, compounds 4 (3-nitro) and 8 (3-chloro) were the only compounds that elicited a dose-dependent decrease in cell viability (IC50 values 9.7 and 33 M, respectively) of HT 29 cells. The same compounds exhibited a significant inhibitory effect on the cell proliferation and colony-forming capability of HT29 cells. Co-administration of compounds 4 and 8 with electron transport chain inhibitors and mitochondrial K+-ATP channel blockers in H9C2 enhanced the anti-proliferative capacity of the compound. Furthermore, Insilco molecular docking studies revealed that the anti-proliferative effect of these compounds could be attributed to interactions with the colchicine-binding site of tubulin. In conclusion, our results demonstrated that novel 1,2,3-triazole-chalcone hybrid can be a potent therapeutic agent against HT-29 cells, and its anti proliferating...
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Posted by admin on Jan 31, 2022 in |
Objective: The present research was focused on designing, formulate and evaluate the trilayer matrix tablets incorporated with quinapril for extending drug release. Methods: Quinapril trilayer matrix tablets were formulated using response surface methodology wherein initially 27 formulations (QF1-QF27) were designed for active layer from which one best formulation was chosen based on drug content, swelling index, and in-vitro release studies. The chosen formulation was formulated into extended-release trilayed matrix tablet by varying proportions of polymers by direct compression technique and was evaluated for various physicochemical parameters, drug release and the drug release data were fitted into the various kinetic model to know the mechanism of drug release. The best-optimized formulation was further characterized by FTIR and stability studies. Results: 27 active layer formulations were evaluated for various physicochemical properties and drug release, out of which the highest drug release was exhibited by QF16 (98.85%). Thus, QF16 was used for formulation into trilayer matrix tablets (AQF16-HQF16). All the formulations were evaluated for drug content, swelling index, and percentage drug release...
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Posted by admin on Jan 31, 2022 in |
Lupeol (I) is a naturally occurring triterpene that has been isolated from the stem bark of Crataeva nurvala in appreciable amount. Due to the presence of a single hydroxyl group and a large, apolar skeleton, lupeol acts as an amphiphile. The two possible sites for chemical modification present in lupeol are ring-A and isopropenyl side chain. We modified it in three naturally occurring analogous derivatives, i.e., 3a, 5a, 5b, 8, 8, 11a-Hexamethyl-1-(2-methyl-oxiranyl)-icosahydro-cyclopenta[a] chrysen-9-ol (II), lupeol acetate (III), and lupenone (IV) by oxidation and acylation process. The structures of the newly synthesized compounds were confirmed by elemental analysis, 1H, 13C NMR, IR, and MS spectroscopy. In-vitro antioxidant activity for all the compounds evaluated where ascorbic acid (vitamin C) treated as standard. All the analysis was made with the use of UV-Visible spectrophotometer. Result of the study suggested that all the compounds showed effective efficacy for antioxidant properties in a concentration-dependant manner, although lupeol acetate was found most significant in comparison to...
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