Design, synthesis and biological evaluation of diarylpyrazole/triazole bearing 1,3,4- oxadiazole moiety as coxs inhibitors endowed with potential anti-inflammatory and analgesic activities

[...]the binding interactions of 13a into the active site of COX-2 isozyme was explained by performing a docking study. [...]the CYP450 pathway that produces different types of eicosanoids including epoxyeicosatrienoic acids (EETs) and 20hydroxyeicosatetraenoic acid (20-HETE)1,2. In the present study, we have substituted the carboxylic acid/amide moieties of 1,5diaryl-heterocyclic cores with the bioisosteric 1,3,4oxadiazole nucleus to study their effect on the activity. [...]the lipophilicity of the prepared compounds was increased through the incorporation of trifluoromethyl aniline and adamantly moieties, in an attempt to improve their COX-2 inhibitory ability (Fig. 2.) The proton/carbon magnetic resonance (1H NMR and 13C NMR) spectra were executed with a Bruker APX400 spectrometer at 400 MHz and 101 MHz, respectively in the specified solvent at the Faculty of Pharmacy, BeniSuef University. [...]5 was outlined on the d scale and J values were recorded in Hz.