Posted by admin on May 31, 2020 in |
Substituted triazoles have received considerable attention during the last two decades as they are endowed with a variety of biological activities and have a wide range of therapeutic properties. The present work is concerned with the synthesis of fused 1, 2, 4-triazole derivatives with the objective of discovering novel and potent anti-tubercular agents that might be devoid of harmful side effects. 1-[amino (isonicotinoyl) carbonohydrazonoyl] guanidine (I) was prepared from isoniazide and cyanoguanidine and was cyclized to 2-(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl) guanidine (II) which was further converted into amino triazolo triazine derivatives (IIIa-g) by refluxing with the appropriately substituted benzaldehydes. The final compounds 10-substituted-2-(pyridin-4-yl)-6,10-dihydro-5H-pyrimido[2,d] [1,2,4] triazolo[1,5-a] [1,3,5] triazine-6-carboxylic acid (IVa-g) were obtained by refluxing different amino triazolo triazine derivatives (IIIa-g) with formaldehyde and sodium pyruvate in presence of HCl in methanolic medium. The newly synthesized compounds were screened for their antitubercular activity using a microplate alamar blue assay method and characterized on the basis of IR, 1HNMR and Mass spectral...
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Posted by admin on May 31, 2020 in |
In folk medicine, especially in developing countries, several plant species are employed for the treatment of snakebites that lack prompt access to serum therapy. Andrographis serpyllifolia (Vahl), belonging to Acanthaceae, has been recorded in ethnobotanical archives as a plant possessing potent anti-ophidic activity for snake bites. The present study emphasis to investigate the phytochemical profile and anti-oxidant properties of various plant extracts of A. serpyllifolia. To carry out this work, various cold plant extracts were prepared from shade dried leaves and used. During qualitative analysis, all the plant extracts showed positive results for all phytocompounds. Various quantitative assays exhibited that all plant extracts were having significant level of secondary metabolites with values ranging from 1148 to 286 mg GAE/g for phenol, 1262 to 976 mg LN/g for terpenoids, 172 to 106 mg RE/g for flavonoids and 21.5 to 3.6 mg TA/g for tannins. All the plant extracts tested had higher DPPH, ABTS scavenging activity, and metal chelating ability. The free radical scavenging activity of plant extracts were found to...
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Posted by admin on May 31, 2020 in |
Nitrofurantoin is a broad-spectrum bactericidal antibiotic that affects both gram-negative and gram-positive bacteria. Nitrofurantoin exhibits bacteriostatic or bactericidal effects by inhibiting the synthesis of DNA, RNA, protein, and cell wall synthesis. Nanocrystals of NFT were prepared by a cold high-pressure homogenization technique. To improve the dissolution rate, the drug was formulated in a nanocrystal by using an emulsion diffusion method, high-pressure homo-genization or sonication. NFT was dispersed in aqueous surfactant solution containing poloxamer 188, PVPK 30, and HPMC E3 under continuous stirring. Poloxamer 188 was used as a surfactant for the preparation of the NCs. Formulation NC9B3 has a mean particle size 231 ± 9 nm with polydispersity index 0.09 ± 0.02, which indicates a very narrow particle size distribution. % Entrapment efficiency was 98.3 ± 0.7 slow drug release profile indicates the homogeneous dispersion of NFT in the lipid matrix. NCs have crystalline nature with rough surfaces, which has been confirmed using SEM analysis. XRPD spectra show the reduction in the crystalline behavior of the drug and the...
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Posted by admin on May 31, 2020 in |
Resistance to antimicrobials by pathogenic bacteria is a global menace. An attractive pathway to resolve this problem of resistance may be achieved by targeting the bacterial quorum sensing (QS) process. Fighting bacterial infections by interfering with their command language and disrupting virulence expression could serve as a viable alternative. One of the current strategies is to attenuate virulence gene expression of agr quorum sensing system of some Gram-positive bacteria through inhibition of AgrA_ P2/P3 interaction. Tertiary structures of AgrA proteins of some pathogenic bacteria like Listeria monocytogenes, Chlamydia trachomatis, Enterococcus faecalis, Streptococcus pyogenes and Macrococcus canis showing antimicrobial resistance are not yet available in structural databases like PDB. These proteins play a key role in AgrA quorum sensing. 3D structures of these proteins are essential to determine most of their functions, and for the development of agents that can be explored as therapeutic agents. In order to derive structures of these AgrA proteins, homology modeling approach was employed. The modeled proteins were validated by several methods, and the physico-chemical...
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Posted by admin on May 31, 2020 in |
Herbal medicine nowadays offers several options to modify the progress and symptoms of medicines. There has been a new trend in the preparation and marketing of drugs based on medicinal plants and their scientific and commercial significance. These plant-derived products are carefully standardized and their efficacy and safety for a specific application have been demonstrated. The objective of this work is to prepare different crude extracts from the leaves of a medicinal plant, Bacopa monnieri through the maceration method and determine their total phenolics, flavonoids and other components and also the antioxidant activity by established methods. The Bacopa monnieri leaves were collected from East Kolkata Wetland, India. The different crude extracts were prepared by using different solvents of different polarities. The total phenolic contents were determined by using the UV visible spectroscopy method. The content of the total phenolic of different leaves crude extracts was in the range of 17.43 mg/g-46.24 mg/g of dry crude extracts. The antioxidant activity was assessed by conventional a-diphenyl-b-s-picrylhydrazyl (DPPH) methods. The highest antioxidant...
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