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VIRTUAL SCREEENING AND PHARMACOLOGICAL EVALUATION OF NEWER BTK INHIBITIORS AS POTENT ANTI-RHEUMATOID ARTHRITIC AGENTS
Rheumatoid arthritis is a chronic autoimmune disease affecting 1% of the world wide population. Recent researches suggested that the need for discovery of new therapeutic disease modifying anti-rheumatoid arthritis drugs (DMARD’s). BTK (Bruton’s tyrosine kinase) is cytoplasmic, non receptor tyrosine kinase and it is efficient target for the treatment of rheumatoid arthritis. This encouraged us...
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PLACKETT-BURMAN SCREENING OF OLMESARTAN MEDOXOMIL LIQUISOLID TABLETS: QUALITY BY DESIGN APPROACH
Solubility is considered as the important parameters to achieve desired concentration of drug in systemic circulation for achieving required pharmacological response. Olmesartan medoxomil (OLM) is poorly soluble belongs to BCS class II. The drug is rapidly absorbed following oral administration, with a bioavailability approximately 26%. Liquisolid technique was used to enhance the aqueousÂ...
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LEAD FINDING FROM WHOLE PLANT OF CURCUMA LONGA WITH OXIDATIVE POTENTIAL
The present study deals with the antioxidant activity, drug likeness score and bioactivity score of the compounds isolated from Curcuma longa and search lead antioxidant compound through molinspiration software. We have taken ten compounds from this plant. All the compounds were further subjected to molecular properties prediction and drug likeness by Molinspirstion and found in compliance with ...
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FORMULATION AND EVALUATION OF STOMACH – SPECIFIC NOVEL GASTRO-RETENTIVE FORMULATIONS OF 5-FLUOROURACIL FOR TARGETING GASTRIC CANCER
Intravenous administration of 5-Fluorouracil (5FU) produces severe systemic, dose-related side effects due to its cytotoxic nature, additionally, 5FU is rapidly absorbed from the stomach after oral administration. Therefore a combined floating-bioadhesive tablet (FBT) of 5FU has been developed in order to reduce the dose and associated side effects in other sites of the body. The tablets were prep...
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PEROXYNITRITE SCAVENGING AND TOXICITY POTENTIAL OF DIFFERENT FRACTIONS OF THE AERIAL PARTS OF BACOPA MONNIERA LINN.
Bacopa monniera is locally referred as Brahmi Shak, has been reputed to use in the Ayurvedic system of medicine for centuries. In our ongoing study to identify the scavenger of ONOO- from natural sources, the aerial parts of Bacopa monniera Linn. was evaluated to scavenge authentic peroxynitrites (ONOO-) and to inhibit total reactive oxygen species (ROS) generation, in kidney homogenates using 2',...
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A STUDY ON PHYSICAL, CHEMICAL, AND ANTIOXIDANT PROPERTIES OF ESSENTIAL OIL SEPARATED FROM FRESH BERRIES OF CINNAMOMUM RIPARIUM BY STEAM DISTILLATION TECHNIQUE
Cinnamomum riparium Gamble belongs to the family Lauraceae is a red listed species by the International Union for Conservation of Nature (IUCN). It is a tree growing in evergreen forests and traditionally used for treating conditions like wound healing, fever, intestinal worms, headache, inflammations, menstrual problems etc. According to tribal’s, this activity is mainly due to the volatile oil...
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SYNTHESIS AND CHARACTERIZATION OF [16]- MEMBERED DIOXA DIAZA NAPTHALDEHYDE BASED MACROCYCLIC LIGAND AND ITS COMPLEXES OF Co(III), Ni(II) AND Cu(II) PERCHLORATE IONS
An hitherto new unreported [16]-membered dioxadiazanapthaldehyde based macrocyclic ligand (L) 2,11-dioxa-23,30-diaza heptacyclo [30.4.0.04,9.012,21.014,19.024,29.034,39] -tetraconta-12,14,16, 18,20,22, 24,26,28,30,32,34,36,38,40-pentadecaene, has been synthesized by two different synthetic routes each involving two stages. 2-Hydroxy-1-Napthaldehyde in the presence of potassium carbonate was trea...
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PULSATILE DRUG DELIVERY OF CANDESARTAN CILEXETIL FOR CARDIOVASCULAR COMPLICATIONS
The aim of current investigation was to formulate and evaluate an oral time controlled drug delivery system to achieve timed release of Candesartan cilexetil for the treatment of cardiovascular complications. Blood pressure rises early in the morning which can leads to hypertension and congestive cardiac failure. Attempt has been made to develop a drug delivery which releases the drug based on cha...
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MOLECULAR DOCKING STUDIES OF ORGANOSULFUR COMPOUNDS AND FLAVONOIDS OF ALLIUM SATIVUM AGAINST EGFR TO TREAT NON-SMALL CELL LUNG CANCER
Lung cancer is one of predominant cancer which leads to death in the developed and developing countries. 80% of lung cancer cases in India are reported as Non-Small Cell Lung Cancer (NSCLC). EGFR (Epidermal growth factor receptor) that belongs to the tyrosine kinase family (RTKs) is the key paradigm of molecular targeted therapy of lung cancer. Garlic (Allium sativum) is a common Indian spice that...
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PHARMACOLOGICAL EVALUATION OF ANTI-ULCER EFFECTS OF COMBINED DOSES OF ALOE VERA AND VITAMIN-E AGAINST INDOMETHACIN INDUCED PEPTIC ULCER MODEL
Peptic Ulcer Disease (PUD) is one of the most prevalent pathogenic conditions which affects around 5-10% of the global population. Helicobacter pylori infection and the use of Non-Steroidal Anti-inflammatory Drugs (NSAIDs) are two of the most common etiological causes in the PUD pathogenesis. First line treatment for PUD involves use of drugs which cause acid suppression or target against the erad...
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