Novel aryl carboximidamide and 3-aryl-1,2,4-oxadiazole analogues of naproxen as dual selective COX-2/15-LOX inhibitors: Design, synthesis and docking studies
A series of novel naproxen analogues containing 3-aryl-1,2,4-oxadiazoles moiety (4B-G) and their reaction intermediates aryl carboximidamides moiety (3B-G) was synthesized and evaluated _in vitro_ as dual COXs/15-LOX inhibitors. Compounds 3B-G exhibited superior inhibitory activity than celecoxib as COX-2 inhibitors. Compounds 3B-D and 3G were the most potent COX-2 inhibitors with IC50 range of 6.4 – 8.13 nM and higher selectivity ... Read more