Posted by admin on Dec 25, 2014 in |
Compounds with a 2(H)-1, 4-benzoxazin-3(4H)-one skeleton have attached the attention of phytochemistry researchers since 2, 4-dihydroxy-(2H)-1,4-benzoxazin-3(4H) and 2,4-dihydroxy-7-methoxy-(2H)-1,4-benzoxazin-3(4H)-one were isolated from plants belonging to the Poaceae family. These compounds exihibit interesting properties11 such as phytotoxic, antimicrobial12, antifeedent, antifungal and insecticidal properties. The reaction of CSI with 2-Chlorobenzyl alcohol result in N-chlorosulphonyl derivatives, which show antibacterial potency. Futher, N-chlorosulphonyl derivatives can be easily cyclofunctionalized. This cyclofunctionalization has been exploited in the synthesis of the title compounds (3). Thus, the title compound being oxygen analogues of 1, 3-thiazine derivatives together with N-sulphonamide moiety could be expected to exhibit enhanced...
Read More
Posted by admin on Dec 25, 2014 in |
Lopinavir (LPV) is potent and poorly bioavailable molecule which is frequently administered protease inhibitors in the treatment of the HIV. Solid Lipid Nanoparticles (SLNs) of LPV were prepared using High Speed Homogenization. LPV were successfully encapsulated in the mixture of Glyceryl Behenate and Glyceryl monostearate. Poloxamer 188 was used as a surfactant for the preparation of the SLNs. Formulation composition and process parameter were optimized to get the desired quality of the SLNs. Formulation PF5 have mean particle size 185 ± 5 nm with Polydispersity index 0.11 ± 0.01 which indicates very narrow particle size distribution. % Entrapment efficiency was 86.2 ± 1.5. Slow drug release profile indicates the homogeneous dispersion of LPV in lipid matrix. SLNs have spherical shape and smooth surface which has been confirmed using SEM analysis. XRPD spectra show the reduction in crystalline behaviour of the drug and the lipid after formation of the SLNs. There was no significant change in the mean particle size and Polydispersity index after 6 month storage at 25°C/60%...
Read More
Posted by admin on Dec 25, 2014 in |
Two simple, precise, accurate and economical visible spectrophotometric methods were developed for the determination of faropenem in bulk and in tablet dosage forms have been described. The method A was based on the formation of green color complex with Potassium ferri-cyanide in the presence of Ferric chloride, which show maximum absorbance (λ max) at 745nm.The method B is based on the reduction of ferric ion into ferrous ion by the drug in the presence of Ferric ammonium sulphate-1, 10-phenanthroline to form a highly stable Orange red colourferrion complex measured at 511 nm. Mean assays of method A and B was found to be 99.9% and 99.4 % respectively. LOD and LOQ of method A was found to be 2.22 μg/ml and 7.44 μg/ml respectively and for method B it was 7.88 and 26.11 μg/ml.The results of analysis for both the methods have been validated statistically as per ICH guidelines. The proposed methods were simple, sensitive and economical for the quantitative determination of faropenem and were successfully employed for the...
Read More
Posted by admin on Dec 25, 2014 in |
In recent years, synthesis and biological evaluation of novel 4H-1, 4-benzothiazines and their sulfone analogues have gained momentum due to their medicinal and industrial importance. The present article describes the synthesis of new 4H-1, 4-benzothiazines via condensation and oxidative cyclization of substituted 2-aminobenzenethiols with compounds containing active methylene groups. It is believed that the reaction proceeds via intermediary of the enaminoketone system. The sulfone derivatives were synthesized by oxidation of 4H-1, 4-benzothiazines using 30% hydrogen peroxide in glacial acetic acid. The structures of the compounds have been confirmed by spectral and chemical analysis.The synthesized compounds were screened for antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay and 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS●+) radical cation decolorization assay. The in vitro antibacterial activity was tested against S. aureus, B. subtilis (Gram positive) and E. coli, Pseudomonas aeruginosa (Gram negative) microorganisms using paper disc diffusion method using nutrient agar medium and the antifungal activity of synthesized compounds was tested on fungal strains: A. niger, C. albicans using disc diffusion...
Read More
Posted by admin on Dec 25, 2014 in |
The main aim of the present study was to synthesize new leads with potential antibacterial and antioxidant activities. As a part of systematic investigation of synthesis and biological activity, some of the new thiazoldinedione compounds 5a-e were prepared and screened for their antibacterial and antioxidant activities. The antibacterial evaluation of newly synthesized compounds was carried out by cup-plate method. Antimicrobial activity results revealed that compound 5a showed promising activity against bacteria Staphylococcus aureus, Klebsiella pneumonia, and Pseudomonas aeruginosa, 5e was found to be more active aganist Proteus vulgaris. The antioxidant activity was performed by using free radical scavenging activity by DPPH (1, 1-diphenyl-2-picryl-hydrazil) assay method and Ferric ion reduction method, ascorbic acid was used as reference standard. All the tested derivatives show antioxidant activity but compound 5c and 5d show promising antioxidant activity concentration at 50μg /ml and can be further studied with modifications. Some novel thiazolidinediones derivatives 5(a–e) were synthesized by reacting hydrazine hydrate in ethanol to form hydrazinecarboxylicacid [4-(2, 4-Dioxo-thiazolidin-5-ylidenemethyl)-phenyl-esterand substituted derivatives were formed by further reaction....
Read More
