MORE COX-2 SELECTIVE INHIBITORS
Design, Synthesis and biological evaluation of some novel indole derivatives as selective COX-2 inhibitors
... their COX- 2 selectivity and reduce their ulcerogenic side effects attributed to their high COX-1 selectivity and the acidic properties of the ...good COX-2 selective ...increase ...
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Cardiovascular and gastrointestinal effects of COX 2 inhibitors and NSAIDs: achieving a balance
... A 2 and prostaglandin I 2 , COX-2 inhibitors selectively suppress the production of prostaglandin I 2 without affecting thromboxane A 2 ...whom COX-2 is ...
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Effects of COX-1 and COX-2 Inhibitors in L- Nitro-L- Arginine Methyl Ester Induced Hypertensive Rats
... by COX-1. On the other hand, COX-2 markedly elevated serum K + level compared with the L- NAME group ...regarding COX-1 related with serum Na + regulation was obtained by Lpez- Parra et ...
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COX SELECTIVE ANTIINFLAMMATORY DRUGS AND ITS DEVELOPMENT
... non selective agent by chang- ing or substituting with different functional groups can effectively increase the activity and selectivity of the drugs as for example, lengthening the carboxyl side chain of ...
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Viscum album-Mediated COX-2 Inhibition Implicates Destabilization of COX-2 mRNA
... Since COX-2 expression is up-regulated during several pathological conditions and human malignancies, strategies controlling the expression and activity of COX-2 have been developed as potent ...
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Should selective Cox-2 inhibitors be used more?
... PERSPECTIVES: SELECTIVE COX-2 INHIBITORS AND THEIR ALTERNATIVES Although, coxibs are widely prescribed drugs due to their stomach-friendly nature, recent controversies regarding their ...
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Reduction in cancer risk by selective and nonselective cyclooxygenase-2 (COX-2) inhibitors
... and selective coxibs should be considered a top cancer research ...priority. Selective and nonselective coxibs are already dispensed on a regular basis to a large population of patients, for the treatment ...
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2D QSAR STUDY OF INDOLE DERIVATIVES AS SELECTIVE COX 2 INHIBITORS
... be more for increasing activity and total van der Waals surface area with negative electrostatic potential of the molecule contributing negatively indicating that negative electrostatic potential on surface should ...
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QSAR Study of 4-Benzylideneamino-Benzenesulfonamides and 4-Phenyliminomethyl-Benzenesulfonamides as Selective Cox-1 and Cox-2 Inhibitors
... the COX-2 selective inhibitor NSAID drugs were thought to be a major breakthrough, with the Expectation of a significant reduction in gastrointestinal (GI) side ...effects. COX-2 is ...
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Synthesis and biological evaluation of 4 (substituted phenylsulfamoyl) 2 hydroxyphenyl acetate derivatives as potent anti inflammatory and selective COX 2 inhibitors
... for COX-1 and COX-2, ...inhibit COX-2 and/or COX-1 using the purified colorimetric COX (ovine) ...(Table 2). In this preliminary study towards new potential ...
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Cyclooxygenase-2 (COX-2) inhibitors: future therapeutic strategies for epilepsy management
... to COX-2 ex- pression may involve regulatory kinases such as SPK, TK, PKC, NF-κB, ERK, and MAPK [58, ...induced COX-2 via ERK, thus mediating astroglial- neuronal interaction to enhance ...
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Synthesis, Cyclooxygenase Inhibition, Anti inflammatory Evaluation and Gastric Liability of Some Novel Indole Derivatives as Selective COX 2 Inhibitors
... SO 2 Me or SO 2 NH 2 group as a pharmacophore of COX-2, exhibited the most anti-inflammatory and selectivity actives so, they were more evaluated by calculating their ED 50 % ...
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Exploring Structural Parameters for Designing Cox 1 and Cox 2 Inhibitors: Pharmacophoric Modeling, Virtual Screening and Docking Study
... as COX-1 inhibitors and 01 bioactive as COX-2 ...selecting more potent hit molecules. The approach of deciding COX- 1/COX-2 selectivity based on binding energy ...
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Synthesis and preliminary evaluation of potential highly selective COX 2 inhibitors of some nonsteroidal anti inflammatory derivatives
... Mohammed Alherwi 1 , Sadik Almekhlafi 2 *, Abdulghany H. Ahmed 3 and Doa’a A. Ibrahim 4 1,2 Department of Medicinal Chemistry, Faculty of Pharmacy, University of Science and Technology, Sana'a, Yemen 3 Department ...
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Discovering COX-2 Inhibitors from Flavonoids and Diterpenoids
... The distribution of energy values after geometry optimization (Fig.4 left) and log P (Fig.4 right) of the ligands (listed in Fig.3) was provided in Fig.4.It could be seen that 88.46% of the ligands used in this work ...
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Microbial Metabolism of Rofecoxib, A Selective COX-2 Inhibitor
... 13 C NMR showed seventeen resonances distributed as one methyl, one methylene, eight aromatic methines, and one oxygenated aromatic quaternary carbon. Other quaternary carbons were almost identical to those of the parent ...
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Selective inhibition of cyclooxygenase (COX) 2 reverses inflammation and expression of COX 2 and interleukin 6 in rat adjuvant arthritis
... inducible COX-2 enzyme to inflam- mation in rat adjuvant arthritis was evaluated by character- ization of COX-2 expression in normal and arthritic paws and by pharmacological inhibition of ...
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A double prodrug system for colon targeting of benzenesulfonamide COX 2 inhibitors
... drugs. 2 The role of COX-2 in the aetiology and progression of the disease is well characterized and the enzyme is an important pharmacological ...The COX-2 inhibitor celecoxib ...
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Cox-2 inhibitors from stem bark of Bauhinia rufescens lam. (Fabaceae)
... ABSTRACT Chemical investigation of the stem bark of Bauhinia rufescens resulted in the isolation of a new cyanoglucoside and menisdaurin from methanol extract and oxepin from petroleum ether extract. The isolated ...
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Combination therapy of PKCζ and COX-2 inhibitors synergistically suppress melanoma metastasis
... of COX-2 is a common character- istic of many human carcinomas. COX-2 plays an im- portant role in tumorigenesis as mediating the progression and metastasis of tumors, such as nasopha- ryngeal ...
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