Posted by admin on Dec 23, 2014 in |
In the present work , novel 2-Amino-N’-(2-oxoindolin-3-ylidene) benzo[d]oxazole-5-carbohydrazides were synthesized and evaluated for In-vivo anti-inflammatory activity by carragenan induced rat paw edema method and were known to exhibit promising anti-inflammatory activity at a dose of 30mg/kg bw. Compounds D2, D3, D5 and D8 were found to be comparatively potent with the standard...
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Posted by admin on Dec 1, 2014 in |
Rheumatoid arthritis is a major ailment among autoimmune disorders. A large number of herbal extracts were used for the treatment of various types of rheumatoid disorder. The leaf and root of Justicia gendarussa belonging to Acanthaceae family, commonly known as Nilinirgundi is traditionally used for chronic rheumatism. The present study deals with in-vitro anti-arthritic activity in pharmacological models were studied such as inhibition of protein denaturation and trypsin (proteinase) inhibitory activity. Different fractions and isolated compound from methanolic extract of leaf and root of J.gendarussa with different concentrations (10,100,1000µg/ml ) were studied and results were compared with standard drug Indomethacin. The methanolic extract of leaf and root of J. gendarussa showed dose dependent activity which was found comparable to that of standard drug Indomethacin. Isolated compound-La of leaf of J. gendarussa inhibited the activity of trypsin with IC50 values 34.85 µg/ml as compared to standard drug Indomethacin with IC50 value 11.57 µg/ml. Compound-La of leaf of J. gendarussa showed protein denaturation inhibition at the IC50 value of 24.74 µg/ml...
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Posted by admin on Dec 1, 2014 in |
This work involves synthesis of pyrazolyl thiazine derivatives from different chalcones [1(a-b)] synthesized from substituted acetophenones and different aromatic aldehydes in basic medium by Claisen-Schmidt reaction. These chalcones [1(a-b)] on condensation with different hydrazides [2(a-b)] and isothiocyanates [3(a-b)] when irradiated with microwaves (20%, 140watts) in scientific microwave oven, give different 2-phenyl-2,5-dihydro-pyrazole-1-carbothioic acid phenyl amide derivatives [4(a-g)] which on further MW assisted condensation with substituted acetophenones and different aromatic aldehydes, furnish pyrazolyl thiazine derivatives [7(a-j)]. Library of such pyrazolyl thiazine derivatives has been generated and the structures were subjected to PASS for their probabilities of being active biologically. QSAR study of the library was done to find out most active...
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Posted by admin on Dec 1, 2014 in |
The objective of present research work is to provide green technique for synthesis of 4-(4-Hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl ester. Pyrimidine derivatives are well known in the pharmaceutical industry and exhibit to possess a broad spectrum of biological activities which makes their wider application as a key building block for pharmaceutical agents. Highly efficient and simple methods complying with principle of Green chemistry have been described in this manuscript for the synthesis with competent yields. As part of current studies, we here in report economical practical techniques like- microwave synthesis, mortal-pastel method (mechanochemistry) and by application of green solvents for the synthesis. On completion of reaction the products were characterized by Infra Red Spectroscopy, Nuclear Magnetic Resonance Spectroscopy and Mass Spectra. The specified methods for synthesis are more convenient and reactions can be carried out in higher yield (80-96%), shorter reaction time (3-30 min) and milder conditions, without generation of pollution and safer to...
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Posted by admin on Dec 1, 2014 in |
The aim of present research work to develop and optimize orodispersible film of baclofen to improve bioavailability and patient compliance. Orodispersible films of baclofen were prepared by solvent casting method using HPMC E5 LV as a film forming polymer and propylene glycol as a plasticizer, crospovidone as a superdisintegrant and sucralose was added as a sweetener. The physical mixture of drug and polymer characterized by FT-IR showed no incompatibility. A 32 central composite design was applied using two independent variables such as X1 (Polymer) and X2 (Propylene glycol) and folding endurance (Y1), T90% (Y2), In-vitro Disintegration time (Y3).The prepared films were evaluated for weight, thickness, folding endurance, disintegration time, in vitro drug release, drug content and their mechanical properties such as tensile strength and % elongation. From the result obtained optimized formulation was prepared with 2.58% w/v HPMC E5 LV and 2.02 % w/v of propylene glycol showed folding endurance of 68.59, disintegration time 53.4 seconds,T90% of 9.12 minutes. A stability study result reveals that there was no significant...
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