关键词: 吡咯里嗪衍生物, 非甾体类抗炎药, 合成

Dual inhibitors of COX and 5-LOX may have synergistic anti-inflammatory effects and reduce the side-effects of COX inhibitors by blocking the formation of both prostaglandins and leucotrienes. In this paper, two series of compounds with pyrrolizine as a template were designed and synthesized as novel COX/5-LOX dual inhibitors, including 5-aroyl-7-aryl-2,3-dihydro-1H-pyrrolizines and 6-aroyl-7-aryl-2,3- dihydro-1H-pyrrolizines, and an efficient synthetic method has been developed for the synthesis of 5- or 6-aroylpyrrolizine. All target compounds have been identified by MS, 1H NMR spectra and elemental analy-sis. The structures and molecular configuration of compound III and IV have been confirmed by NMR spectra.

Key words: pyrrolizine derivative, synthesis, non-steroidal anti-inflammatory drug