The receptor was docked to the commercially availableantiviral agents that have broad serotype specificity. This family of antiviral agents Arildone was found to have limited antiviral activity by using ProteinStructure Modeling Method, using INSIGHTII software. We tried to improve the binding efficiency and steric compatibility of Arildone against Rhinovirus. Several modifications were made to the probable functional groups which were interacting with receptor molecule. Analogs of the drug molecule were prepared using MODELLER9v1chemsketch and docked using INSIGHT II docking software. The modified drugs was sketched using chemsketch were found to be better than the convectional drugs available. Further from this work we can improve the steric compatibility and then Absorption, Distribution, Metabolism and Excretion (ADME) properties of the analogs can be analyzed using Insilco ADME tools.
M. Shankar*, M. Niranjan Babu, Pranabesh Sikdar, E. Mohana Roopa.
A validated reverse phase HPLC method has been developed for the simultaneous estimation of ibuprofen and codeine phosphatein Pharmaceutical dosage forms. The chromatographic separation was carried out on Kromasil 100, C18, 5 micron (250 x 4.6 mm) column at Ambient temperature (25oC) and Buffer: Acetonitrile (gradient) was used as mobile phase at the flow rate of 1 ml/min with PDA detection at 220 nm. The retention time of ibuprofen and codeine phosphate were found to be 18.003min and 9.676 min respectively. Linearity of both drugs were found to be in the concentration range of 360-480 µg/ml for ibuprofen and 20.48-30.72 µg/ml for codeine phosphate. The developed HPLC method was validated by determining its sensitivity, selectivity, linearity, accuracy and precision. The accuracy of the method was assessed by percentage recovery studies at three different levels at 80%, 100% and 120% of its working concentration. The percentage recovery of both drugs in the developed method was found to be in the ranges of from 98.5-101% that indicates the good accuracy of the method. This developed method can be used for the routine analysis for the estimation of ibuprofen and codeine phosphate in tablet dosage form.
A simple, sensitive, economical and validated method is developed using LC-MS/MS with electro spray ionization for the quantification of Duloxetine in human plasma. Following protein-precipitation extraction, Separation of analyte and internal standard (Telmisartan) was performed on X-Bridge (4.6 x 50 mm, 3.5µm) column using a gradient elution mode were run in positive mode using Telmisartan as IS with mobile phase composition of 100% methanol and 0.1% formic acid on a reverse phase column and analyzed by MS /MS (API 4000) in the multiple reaction monitoring mode using the respective [M+H] + Ions, m/z 297.90 to 154.1 for Duloxetine and m/z 515.10 to 276.30 for IS. The assay exhibited a linear dynamic range of 0.5 to 200 ng/ml for Duloxetine in human plasma. The lower limit of quantification was 0.345 ng/ml with the relative standard deviation between 1.19% to 13.12 (n=6). Acceptable precision and accuracy were obtained for concentrations over the standard curve range. No significant degradation was observed for Duloxetine in human plasma when stored at room temperature (4h), when subjected to Freeze and thaw cycles (3 cycles). The overall absolute recovery is 73 % to 100%. No matrix suppression was found in the method. Because of less run time of 1.3 minutes per sample.
K. Bhanupriya*, Savithri shivakumar, A. Ravi, K.V. Ramanjaneyulu, P. Venkateswara rao, A.M.S. Sudhakar babu.
Ten new 2-oxo-N1-[(E)-quinolin-3-ylmethylidene]-2H-chromene-3-carbo hydrazones(NS 1-10)were synthesized by the reaction of substituted the 2-oxo-2H-chromene-3-carbohydrazide in N, N-dimethyl form amide various 2-Chloro,2-hydr oxy,2-thione-3-formyl quinolines and tetrazolo[1,5-a]quinoline-4-carbaldehyde in presence of catalytic amount of glacial acetic acid. Newly synthesized compounds were characterized by spectroscopic and physical methods. All the synthesized com pounds were screened for antimicrobial by standard methods. Results of the activities reveal that, some compounds exhibited moderate to good anti-microbial activities.
K. Sheeja devi*, G. Beula priyanka, T. Arul salomon, S. Bhagya lakshmi, P. Vijaya kumar, M. Suchitra.
The present work of quinazolinone derivatives were synthesized by treating 2-Chloro-N-(4-oxo-2 phenylquinazolin-3(4H)- (I-1)yl) acetamide with the different substituted phenols in presence of different catalyst like anhydrous potassium carbonate & catalytic amount of potassium iodide in dry acetone. The synthesized compounds have been established on the basis of their m.p., TLC, IR and NMR data. All the newly synthesized quinazolinone derivatives were evaluated for their antibacterial activity by cup plate method by measuring inhibition zone. Gentmycin was used as standard drug. The compound Q-2 showed more potent antibacterial activity than the standard drug Getamycin.
Nagaraju Gollapalli*, J. Naroop Teja, V. Manjusha, M. Srinivasarao, B. Poornima.
A simple, accurate, precise, sensitive and a highly selective spectrophotometric method was developed and validated for the estimation of Zidovudine in bulk and pharmaceutical dosage forms. The stock solutions were prepared as per procedure and were scanned at maximum absorbance of 265 nm. The linearity was found in the concentration range of 2.5-15 μg / mL. The Coefficient of determination (r2) was 0.999. The regression equation was found to be Y = 0.062X + 0.0205 and % RSD was found to be 0.052. The developed method was validated according to ICH guidelines and was found to be simple, accurate and precise. The validation parameters are linearity, accuracy, precision, limit of detection, limit of quantitation, robustness and ruggedness. Thus the proposed method can be successfully applied for the estimation of Zidovudine in bulk and pharmaceutical dosage forms.
B. Prathap*, Akalanka Dey, G. Srinivasa Rao, S. Jeganath, D. Kalyani.