Preparation of New l-(4-Sulfonamidophenyl)-5-aryl-1,2,3-Triazole5-14C Derivatives As COX-2 Selective Inhibitors

摘要

Introduction: Two isoforms of cyclooxygenase (COX) enzyme have been identified1. Non-selective inhibition of these enzymes with non-steroidal anti-inflammatory drugs (NSAID_s) is often accompanied by GI and renal side effects. Selective inhibition of COX-2 would constitute a novel approach to the treatment of inflammation with diminish side effects.Based on the Structures Activity Relationship for selective COX-2 inhibitors the following compounds were designed and labelled with carbon-14 in order to elucidate the mechanism of action and metabolism studies. The desired products, were synthesized according to the synthetic pathway shown in following Scheme.