Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors

2006 ◽  
Vol 16 (17) ◽  
pp. 4483-4487 ◽  
Author(s):  
Latifeh Navidpour ◽  
Mohsen Amini ◽  
Hamed Shafaroodi ◽  
Khosrou Abdi ◽  
Mohammad H. Ghahremani ◽  
...  
Keyword(s):  
Cyclooxygenase 2 ◽  
Water Soluble ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Cox 2 Inhibitors ◽  
Derivatives Of

Design and synthesis of acyclic triaryl (Z)-olefins: a novel class of cyclooxygenase-2 (COX-2) inhibitors

2004 ◽  
Vol 12 (22) ◽  
pp. 5929-5940 ◽  
Author(s):  
Md. Jashim Uddin ◽  
P.N. Praveen Rao ◽  
Edward E. Knaus
Keyword(s):  
Cyclooxygenase 2 ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Cox 2 Inhibitors

Design and synthesis of [ 125 I]Pyricoxib: A novel 125 I-labeled cyclooxygenase-2 (COX-2) inhibitors

2016 ◽  
Vol 26 (6) ◽  
pp. 1516-1520 ◽  
Author(s):  
Ole Tietz ◽  
James Dzandzi ◽  
Atul Bhardwaj ◽  
John F. Valliant ◽  
Frank Wuest
Keyword(s):  
Cyclooxygenase 2 ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Cox 2 Inhibitors

Selective Cyclooxygenase-2 (COX-2) Inhibitors Used for Preventing or Regressing Cancer

2009 ◽  
Vol 4 (2) ◽  
pp. 157-163 ◽  
Author(s):  
Ricardo Pereira
Keyword(s):  
Cyclooxygenase 2 ◽  
Cox 2 ◽  
Cox 2 Inhibitors

scholarly journals Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3550
Author(s):  
Katharigatta N. Venugopala ◽  
Sandeep Chandrashekharappa ◽  
Christophe Tratrat ◽  
Pran Kishore Deb ◽  
Rahul D. Nagdeve ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Graphical Representation ◽  
Hydrophobic Interactions ◽  
Basis Set ◽  
Monoclinic Crystal ◽  
X Ray ◽  
Cox Inhibitors ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Cox 2 Inhibitors

The cyclooxygenase-2 (COX-2) enzyme is an important target for drug discovery and development of novel anti-inflammatory agents. Selective COX-2 inhibitors have the advantage of reduced side-effects, which result from COX-1 inhibition that is usually observed with nonselective COX inhibitors. In this study, the design and synthesis of a new series of 7-methoxy indolizines as bioisostere indomethacin analogues (5a–e) were carried out and evaluated for COX-2 enzyme inhibition. All the compounds showed activity in micromolar ranges, and the compound diethyl 3-(4-cyanobenzoyl)-7-methoxyindolizine-1,2-dicarboxylate (5a) emerged as a promising COX-2 inhibitor with an IC50 of 5.84 µM, as compared to indomethacin (IC50 = 6.84 µM). The molecular modeling study of indolizines indicated that hydrophobic interactions were the major contribution to COX-2 inhibition. The title compound diethyl 3-(4-bromobenzoyl)-7-methoxyindolizine-1,2-dicarboxylate (5c) was subjected for single-crystal X-ray studies, Hirshfeld surface analysis, and energy framework calculations. The X-ray diffraction analysis showed that the molecule (5c) crystallizes in the monoclinic crystal system with space group P 21/n with a = 12.0497(6)Å, b = 17.8324(10)Å, c = 19.6052(11)Å, α = 90.000°, β = 100.372(1)°, γ = 90.000°, and V = 4143.8(4)Å3. In addition, with the help of Crystal Explorer software program using the B3LYP/6-31G(d, p) basis set, the theoretical calculation of the interaction and graphical representation of energy value was measured in the form of the energy framework in terms of coulombic, dispersion, and total energy.

Design, syntheses, and evaluation of 2,3-diphenylcycloprop-2-en-1-ones and oxime derivatives as potential cyclooxygenase-2 (COX-2) inhibitors with analgesic-antiinflammatory activity

2002 ◽  
Vol 57 (1) ◽  
pp. 6-17 ◽  
Author(s):  
Huiying Li ◽  
P.N. Praveen Rao ◽  
Amgad G. Habeeb ◽  
Edward E. Knaus
Keyword(s):  
Antiinflammatory Activity ◽  
Cyclooxygenase 2 ◽  
Cox 2 ◽  
Oxime Derivatives ◽  
Cox 2 Inhibitors

Design and synthesis of new 1,4,5-trisubstituted triazole-bearing benzenesulphonamide moiety as selective COX-2 inhibitors

2021 ◽  
Author(s):  
Mohamed S. Bekheit ◽  
Hanan A. Mohamed ◽  
Bakr F. Abdel-Wahab ◽  
Marwa A. Fouad
Keyword(s):  
Design And Synthesis ◽  
Cox 2 ◽  
Cox 2 Inhibitors

scholarly journals Specific cyclooxygenase-2 (COX-2) inhibitors

1999 ◽  
Vol 99 (6) ◽  
pp. 322 ◽  
Author(s):  
Bernard R Rubin
Keyword(s):  
Cyclooxygenase 2 ◽  
Cox 2 ◽  
Cox 2 Inhibitors

Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors

2014 ◽  
Vol 24 (8) ◽  
pp. 1958-1962 ◽  
Author(s):  
Kyung Ju Kim ◽  
Min Ji Choi ◽  
Ji-Sun Shin ◽  
Minju Kim ◽  
Hye-Eun Choi ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cyclooxygenase 2 ◽  
Docking Analysis ◽  
Cox 2 ◽  
Cox 2 Inhibitors
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