哌嗪衍生物的合成及二肽基肽酶-4活性研究(英文)

Synthesis and biological evaluation of piperazine derivatives on dipeptidyl peptidase-4

本文经过微波辅助1,2,4,5-四氟苯与无水哌嗪的亲核取代反应、甲酰化反应和缩合反应合成了一系列具有潜在二肽基肽酶-4(DPP-4)抑制活性的(4-(2,4,5-三氟苯基)-1-哌嗪基)甲酮衍生物(9a–k),并测定了11个新化合物的DPP-4抑制活性。体外活性测定显示,化合物9d和9g对DPP-4酶具有一定的抑制活性。

A series of （4-（2,4,5-trifluorophenyl）piperazin-1-yl） methanone derivatives 9a–k as potential dipeptidyl peptidase-4 （DPP-4） inhibitors were synthesized by microwave assisted nucleophilic substitution of 1,2,4,5-tetrafluorobenzene with piperazine, followed by carbamoylation and condensation. The inhibitory activities of these new compounds on DPP-4 were evaluated in vitro, and compounds 9d and 9g showed moderate inhibitory activities.