Design, synthesis and evaluation of tetrahydropyran based COX-1/-2 inhibitors.

摘要

Chiral tetrahydropyrans were designed and synthesized by allylations of enantiomerically enriched beta-hydroxy ketones followed by iodocyclisations and nucleophilic replacement of iodo group with C(2)H(5)S(-) and SCN-. In vitro COX-1/-2 inhibitory activities and the docking studies of these compounds identify some of them as moderate inhibitors of COX-1 and COX-2 enzymes.