Posted by admin on Mar 31, 2021 in |
In the present work, a series of some novel substituted benzimidazole derivatives were efficiently synthesized, and a thin layer chromatography study confirmed the completion of the reaction on silica gel-G plates. The characterization was done through recording spectra of FTIR using Jasco FTIR-460 plus spectrophotometer, recording spectra of 1HNMR with the help of spectrometer, specifically BRUKER 400MHz. The synthesized substituted novel benzimidazole derivatives were screened for their in-vitro antitubercular activity by the Microplate Alamar Blue Assay (MABA) method against Mycobacterium tuberculosis (H37Rv strain) with their 2D-QSAR studies. The antitubercular activity results confirmed that compounds DPK3d1, DPK2d1, DPK2d2, DPK2d3, DPK4B1d2, DPK4B2d1, and DPK4B2d2 had shown potent antitubercular activity as compared to standard drugs. These synthesized derivatives were selected 2D-QSAR analysis with their different models such as multiple linear regression (MLR), and partial least squares regression (PLR) analysis were generated to find out the correlation between physicochemical properties parameters and their biological activity. 2D-QSAR models such as MLR and PLS method studies generated an equation showing that descriptors SsOHcount, Ipc Average,...
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Posted by admin on Mar 31, 2021 in |
The primary purpose of this study was to formulate a mucoadhesive vaginal tablet of clindamycin phosphate. It developed to achieve an excellent therapeutic effect and patient compliance in the treatment of bacterial vaginosis. The formulation has a sustained-release effect with good mucoadhesion due to mucoadhesive polymers like Polycarbophil and Carbopol 971P NF, which decreases dose frequency. The mucoadhesive vaginal tablets were prepared by the direct compression method. FTIR had employed to study drug excipient incompatibility. The analytical method performed using HPLC. Optimization of the formulation was done by 32 full factorial designs using DOE. The mucoadhesive vaginal tablet was evaluated for % swelling index, Muco-adhesive strength, drug content, % drug release, and ex-vivo mucoadhesion time. The ex-vivo mucoadhesion time of optimized batch was up to 9 h, 97.24% drug content, 88.34 ± 0.97% drug release observed at 8 h. Stability study shows developed mucoadhesive intravaginal tablet was stable at 30 °C ± 2 °C at 65 ± 5% RH (Room temperature) and 40 °C ± 2 °C at 75...
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Posted by admin on Mar 31, 2021 in |
Impurity profile study is critical for getting market approval of finished dosage forms from regulatory authorities. There are many manufacturing firms (small and medium scale) in India that they cannot afford the high priced USP reference standards for analysis. So, the availability of cheaper affordable IP reference standards will help them adhere to quality guidelines for active pharmaceutical ingredients (APIs) and drug products and assure safe manufacturing system and marketing of pharmaceutical products. This research work is mainly envisaged towards increasing the list of Indian Pharmacopeia (IP) approved impurity reference standards. This paper describes our efforts towards the synthesis and process optimization of the synthesis of cilostazol impurity A. The objective of the present work was to develop a simple route of synthesis that gave a high purity product with good process efficiency. The synthesized cilostazol impurity A was characterized using sophisticated analytical techniques like Fourier-Transform Infrared spectroscopy (FTIR), Nuclear Magnetic Resonance (NMR) and Liquid Chromatography Mass spectrometry (LC-MS). The results indicated that cilostazol impurity A was obtained in...
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Posted by admin on Mar 31, 2021 in |
Jimson weed (Datura stramonium) members of the Solanaceae plant family; serve as major folklore medicinal herbs. The biologically active compounds spectrum in leaves of Datura stramonium L. was investigated by GC-MS with NMR & FTIR analysis. Steroids, terpenoids, anticholinergic alkaloids, atropine, and scopolamine, are detected. Twenty of them are new constitutions for the species, and eight phytosterol compounds are described for the first time. This is the first report on some other antibacterial heterocyclic compounds, antioxidant flavonoids, antimicrobial phytol, amino acids, and sulfone & fluoro compounds in Datura stramonium leave identified by GC-MS...
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Posted by admin on Mar 31, 2021 in |
We presented an eco-friendly procedure for effective and fast preparation of biologically active substituted pyrimidine ligand through a condensation reaction of 1,8-diaminonaphthalene and 2-methoxy-benzaldehyde with Fe3O4@SiO2@L-valine magnetic nanoparticles (MNPs) as a new recyclable catalyst. In this experiment, we aim to increase reaction efficiency for the synthesis of 2-(2-methoxyphenyl)-2,3-dihydro-1H-perimidine ligand. Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), Energy dispersive X-ray spectrometer (EDXA), scanning electron microscopy (SEM), and vibrating sample magnetometry (VSM) were employed to characterize the catalyst. Findings demonstrated that synthesized nanocatalyst is superparamagnetic with a dimension range of 15-30 nm. The catalyst was readily recycled using an external magnet and could be recovered several times without considerable reduction in its catalytic performance. Furthermore, the metal complexes were produced from 2-(2-methoxyphenyl)-2,3-dihydro-1H-perimidine ligand. Antibacterial activities of ligand and its metal complexes were studied against G(+) and G(-) bacteria strains by disc diffusion technique. Results showed that metal complexes had better biological activities compared to parent ligands. Among the synthesized compounds, the best antibacterial activity was observed by Cu...
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