In silico investigation of novel 5-benzylidene-2- (arylsulfonylhydrazono)thiazolidine-4-ones as potential inhibitors of mPGES-1 and COX-2.

Design, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

Synthesis, Anti-Inflammatory and Anti- Nociceptive Activities and Cytotoxic Effect of Novel Thiazolidin-4-ones Derivatives as Selective Cyclooxygenase (COX-2) Inhibitors

  Objective(s): Nowadays, COX- 2 inhibitors such as valdecoxib are removed from the market because of their cardiovascular toxicity and their potential to increase the risk of strokes. In response to this, medicinal chemists have attempted to synthesize new classes of COX-2 Inhibitors.   Materials and Methods: In this study, three novel analogues of thiazolidin-4-ones derivatives ...

Design, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

Synthesis Of 2-[4-(Substituted Benzylidene)-5-Oxo-4,5-Dihydro-Oxazol-2-Ylmethyl]-Isoindole-1,3-Dione Derivatives as Novel Potential Antimicrobial Agents

In the present study, a series of new substituted oxazolone derivatives (4a-4h) were synthesized by the Erlenmeyer condensation of phthaloylglycylglycine with different aldehydes in the presence of anhydrous sodium acetate and acetic anhydride. The structure of newly-synthesized compounds were evaluated by elemental analyses and spectral ( UV-Visible, IR, NMR, Mass) studies. All the synthe...

design and synthesis of novel (e)-2-(4-fluorophenyl)-2-(hydroxyimino)-1-(2-(methylthio)pyrimidin-4-yl)ethanone as potential protein kinase inhibitors and identifying cytotoxic effect