1. | INSILICO SCREENING OF BENZYLIDINE DERIVATIVES OF PYRAZOLONE AS ANTI VIRAL SCAFFOLD |
| Jyothi Achuthanandhan*, Ayana Shaju, Shifana Abdul Muthalif, Kumar P, Safiya Bhava, Reshma Chandran and Baskar Lakshmanan |
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Flavivirus belonging to the flaviviridae family is an important human pathogen, especially in the tropical and subtropical parts of the world, causing considerable morbidity and mortality. They are transmitted by arthropods, especially mosquitoes. It is the peek time when we need to develop an antiviral agent targeting the viral replication. The incidence of vector borne diseases has grown rapidly and human inhabitants are at risk of becoming infected by virus. No specific therapeutic agent has yet been proved for the treatment or prevention of dengue virus. The present study by in silico method focus on exploring the inhibitors of the NS5 RNA dependent RNA polymerase enzyme. The ns5 protein plays as important key enzyme because of the presence of its N-terminal methyltransferase (MTase) and C-terminal RNA-dependent-RNA polymerase (RdRp) domains which are the main targets of antivirals. Design and synthesis of noval compounds have become an important aspect in the field of drug discovery. Hence we have made an attempt to design computationally drugs against dengue virus using pyrazolone derivatives. Key words : NS5 Protein, Pyrazolone, Anti Viral, PDBCode: 4C11and Molecular Docking.
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2. | SYNTHESIS OF MANNICH BASES OF DESLORATADINE USING DIFFERENT TYPES OF ACTIVATED METHYLENE AROMATIC COMPOUNDS AS CYTOTOXIC AGENT |
| Sumaiya Khan*, Md. Mahtabur Rahman , Md. Rabiul Islam |
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The aim of this research is to synthesize Mannich bases of Desloratadine, a tricyclic H1-antihistamine that is used to treat allergies and an active metabolite of loratadine, with activated methylene aromatic compounds. Pharmacological activity of the Mannich bases are tested by brine shrimp lethality bioassay. All of the synthesized compounds were characterized by the use of IR, 1H-NMR, 13C-NMR and Mass spectral data analysis. LD50 values have been determined to establish SAR of the series. Mannich bases of Desloratadine 2a, 2b, 2c, 3 showed moderate to weak cytotoxic activity. Among the synthesized compounds, Mannich base (3) of Desloratadine with 2'-fluroacetophenone showed the highest cytotoxic activity with LD50=1.2, whereas Mannich base (2a), with 4'-chloroacetophenone; LD50=2.3 showed less cytotoxicity. Keywords: Mannich base, Desloratadine, Antihistamine drug, Cytotoxicity, Structure-Activity Relationship
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3. | ANALYTICAL METHOD DEVELOPMENT AND VALIDATION BY NEW RP-UPLC METHOD FOR THE DETERMINATION OF VOXILAPREVIR IN TABLET DOSAGE FORM |
| M. Purushothaman* , P. V. Murali Krishna , Rajesh Asija |
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A simple accurate, precise rapid isocratic RP-UPLC method development for the simultaneous estimation of Voxilaprevir in tablet dosage form. The chromatographic system was carried on Acquity BEH C18 (50*3.0mm. 1.7µm) using mobile phase consisting a mixture of 60 volumes of Methanol of 20 volumes of 0.1% Orthophosphoric acid, 20 volumes of Acetonitrile with detection of 245 nm. The retention time of Voxilaprevir was found to be 1.328 min calibration curve was linear over the concentration range of Voxilaprevir, the correlation coefficient for both peaks were found to be 0.998 respectively. All the analytical validation parameters were determined and found in the limit as per ICH guidelines.
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4. | ANALYTICAL METHOD DEVELOPMENT AND VALIDATION BY NEW UPLC METHOD FOR THE DETERMINATION OF TOLCAPONE IN TABLET DOSAGE FORM |
| M. Purushothaman* and A. Srikanth |
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A simple accurate, precise rapid isocratic RP-UPLC method development for the simultaneous estimation of Voxilaprevir in tablet dosage form .The chromatographic system was carried on Acquity BEH C18 (50*3.0mm. 1.7µm) using mobile phase consisting a mixture of 60 volmes of Methanol of 20 volumes of 0.1% Orthophosphoric acid, 20 volumes of Acetonitrile with detection of 245 nm. The retention time of Voxilaprevir was found to be 1.328 min calibration curve was linear over the concentration range of Voxilaprevir, the correlation coefficient for both peak was found to be 0.998 respectively. All the analytical validation parameters were determined and found in the limit as per ICH guidelines. Keywords: Tolcapone, UPLC
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5. | SYNTHESIS AND STUDIES ON SOME NOVEL DERIVATIVES OF A FUSED HETEROCYCLIC SYSTEM |
| G.Rathinavel*and K.L.Senthilkumar |
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Isoniazid condensed with different derivatives of acetophenone to form hydrazones, using Vilsmeier-Haack reagent to form free aldehyde. The free aldehyde reacts with different free amide (R-NH2) group to form imines(C=N) which on react with Chloro acetyl chloride and Triethylamine to gives Azetidin-2-one derivatives. The structures of the newly synthesized compounds have been established on the basis of their spectral data and elemental analysis. Selected compound were evaluated for antibacterial activity. Keywords: Azetidin-2-one, Vilsmeier-Haack Reagent, Imines and Free Amine Compounds.
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6. | ANALYSIS OF THE CHEMISTRY OF Acacia pycnantha FOR ITS DIURETIC ACTIVITY |
| S. Seshaiah*, M. Madhubhushan, J. Chandrudu, R. Sagar |
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Diuretics play an important role in pulmonary disease and in HTN. Diuretics are determined based on the water output. The mostly used diuretic drugs are thiazides, mannitol, furosemide, ethacrinic acid. These drugs are used in CHD, pregnant toxemia, HTN, diarrhea, menstrual problem and nephritis and also inflammation of the muscles. Different number of plants as traditional medicine performs diuretic activity on animals which are used to treat diuresis. In our study, no lethality was observed at least for the dose and duration used. However, advanced toxicological studies remain to be performed in mice and rats. On basis of the above results, we can conclude that MEAP treatment produced a marked diuresis when rats were acutely treated.
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7. | STANDARDIZATION AND ANALYSIS OF AYURVEDIC FORMULATION |
| R. Shankar Sheshu*, Srikanth A, Shiva Kumar Tejavath, S. Selva Kumar |
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Ayurveda is most commonly used in India which is a natural health care system. The developed countries are mostly using ayurvedic medicines and also cosmetics which are prepared with a your vedic ingredients and nutraceuticals. The ayurvedic plants are identified and properly grown for the preparation use. The physicians and pharmacists should have thorough knowledge in safety and effectivity formulations in patients who are highly using this herbal components. These herbal preparations are not standard and not estimated the quality in the market. In the present investigation, the quality of formulated arista, Kanakarishtam has been accessed. The present findings have shown that all the standard parameters based on which the standardization was carried out, were under acceptable limit as compared to pharmacopoeial specifications. Further, clinical assessment is to be carried out to completely mark the product as “safe and effective”.
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