Posted by admin on Sep 30, 2019 in |
Objective: State of the art, robust and environmentally benign stability indicating assay method (SIAM) has been developed for model drug Edoxabantosylate (EDO) Methods: Successful RP-HPLC chromatographic method was accomplished on a CHROMBUDGET® 100-5-C18 column (250 mm × 4.6 mm, 5 μ) column using methanol and acetate buffer in the ratio of 53:47 having 2.9 pH and 10mM buffer strength. The degradation study was performed in the presence of various stressors, and SIAM develop was selective enough to discriminate the EDO peak with the peak of other degradation production (DP) with acceptable resolution. The degradation kinetics study and fragmentation pattern of isolated major DPs were carried out. Results: The developed SIAM validated as per ICH Q2(R1) guidelines. Two major DPs i.e. DP-I and DP-II, were isolated and characterized thoroughly. Furthermore, the reaction kinetics data revealed that EDO degradation was following first-order degradation kinetics. Conclusion: An extensive stress degradation study along with degradation kinetics, were performed. All probable degradation pathways were predicted by using LC-MS/MS and NMR data obtained by characterization...
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Posted by admin on Sep 30, 2019 in |
This study was performed to identify the antimicrobial compounds in Abies webbiana leaves. The antimicrobial compounds were identified by LCMS-MS. The microbial inhibitory activity was evaluated on Staphylococcus aureus ATCC 6538 using REMA technique and Agar-overlay TLC bioautography. The chloroform extract of Abies webbiana leaves was used for the study. The MIC against Staphylococcus aureus was found to be 195.3 µg/ml- 390.6 µg/ml. A mobile phase comprising of toluene: ethyl acetate: glacial acetic acid (9:1:0.3) was used for identification of antimicrobial compounds present in the extract by TLC bioautography. Totally 16 bands were observed in the HPTLC chromatogram when the plate was observed at 254 nm. The band observed at Rf = 0.58 showed the antimicrobial activity. Preparative TLC technique was used to isolate this active band. The compounds present in the isolated band were then identified by LC-QTRAP. Totally 7 compounds were identified to be present in the isolated bands of chloroform extract. The compounds identified include Betuloside, 2,7-Dihydroxy-4’-methoxyisoflavone, Geinstein 7-O-beta-D-glucoside, β-Sitosterol, Abietane, Coniferol, and 1-(3,4-Dihydroxyphenyl)-1-decene-3,5-dione-Pos. This study...
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Posted by admin on Sep 30, 2019 in |
Schiff bases of isatin are investigated overtime for their pharmaceutical properties and have been found to have various activities such as anti-viral, anti-bacterial, anti-inflammatory, analgesic, anti-HIV, anti-depressant, anti-convulsant, fungicidal, etc. Isatins are treated with hydrazine derivatives and cyclized by sulfuric acid. These compounds are alkylated by di alkyl aminoalkyl halides in specific catalysed conditions. In this study we focus on 4-([1,3,4]oxadiazino[6,5-b] indole-3-yl)aniline derivatives for anti-bacterial activity. Based on literature, glucoseamine-6-phosphate synthase (PDB ID: 2VF5) and dihydropteroate synthase (PDB ID: 1AJ0) enzymes are chosen as potential targets as showed activity for antibacterial and antifungal agents. The in-silico studies were carried out using Swiss ADME and Molinspiration in-silico tools and scoring of molecular docking i.e., virtual screening was done by using AutoDock v.4.0. The in-vitro studies were carried out in the lab using cup-plate method and the zone of inhibition (in mm) was measured. The in-silico results were compared with that of in-vitro and a comparison was drawn. The activity of the compounds was found to have...
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Posted by admin on Sep 30, 2019 in |
In this study, the in-vivo toxicity of Centella asiatica & Evolvulus alsinoides were evaluated by acute and sub-acute toxicity assays according to the guidelines of OECD 423 & 407 respectively. For LD50 evaluation, a single dose of hydro-alcoholic extracts of both plants was orally administered to Swiss albino mice at doses of 200, 400, 800, 1600 and 2000 mg/kg. Then the animals were observed for 72 h. For acute toxicity evaluation, a single dose of hydro-alcoholic extracts of both plants was orally administered to mice at doses of 300, 600, 1200 and 2000 mg/kg. Then, the animals were observed for 14 days. In the sub-acute study, the extracts were orally administered to mice for 28 days at doses of 300, 600, 1200, and 2000 mg/kg. To assess the toxicological effects, animals were closely observed on general behavior, clinical signs of toxicity, body weight, food, and water intake. At the end of the study, it was performed biochemical and hematological evaluations, as well as histopathological analysis from the following organs: brain, heart, liver, and...
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Posted by admin on Sep 30, 2019 in |
Glycosyl isothiocyanates have been widely used as important intermediates in the synthesis of many biologically active glycosyl derivatives. The glycosyl isothiocyanates have been the focus of synthetic attention during recent years because of their potential pharmacological properties. Thiourea and their derivatives are important versatile reagent in organic synthesis and show strong antibacterial activity. Hence, in view of applications of N-glycosylated compounds in medicinal chemistry and in many other ways, we herein report the synthesis and antimicrobial studies of novel glycosyl thiocarbamides of amino tetrazole and aminopyrimidine. In present investigation, a series of novel protected glycosyl heterocycles were synthesized by reaction of glycosyl isothiocyanate with amino tetrazole and amino pyrimidine. The newly synthesized compounds were characterized on the basis of IR, 1HNMR and Mass spectral studies. Antimicrobial evaluation of the synthesized substituted thiocarbamides is also carried out. Antimicrobial activities of the synthesized compound were evaluated against bacteria E. aerogenesa, B. megaterian, S. marcescens, and M. luteus and Fungi A. niger and Penicillinium. All the newly synthesized glycosyl thiocarbamides exhibit promising...
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