Chimie médicale

Novel Fluorescent Derivative of Praziquantel Interaction with Clonorchis sinensis Cercariae

Abstract

Lvyin Zheng, Yunzhi Xie, Wei Liu, Yongquan Wu, Xun Li, Yibao Li and Xiaolin Fan

Clonorchiasis is a common infection of dogs and other fish-eating carnivores (reservoir final hosts). Praziquantel is the only medicine, which has been recommended by WHO for treatment of clonorchiasis. To investigate the interaction between praziquantel and Clonorchiasis sinensis cercariae, two praziquantel derivatives (PZQ-2 and PZQ-3) and one praziquantel fluorescent derivative (PZQ-5) were have been synthesized and characterized by nuclear magnetic resonance spectroscopy (NMR) and MS spectra. Confocal fluorescence microscopy revealed that PZQ-5 is mainly located at cercarial tegument, which leads to the death of cercariae with the time increasing.