Novel Aminoalcohol Derivatives Bearing 4-Phenylphenol as Antischistosomal Drugs

作者：Duan Li Ping; Xue Jian; Tao Yi; Zhang Hao Bing^*

来源：Letters in Drug Design and Discovery, 2012, 9(7): 694-697.

• Aminoalcohol
• 4-phenylphenol
• Schistosoma japonicum
• Drug

There is a need to develop new antischistosomal compounds when the only available therapeutic agents praziquantel large-scale used in the world. A series of novel aminoalcohol derivatives bearing 4-phenylphenol moiety were designed and synthesized. The structures of all the newly synthesized compounds were identified by elemental analysis, H-1-NMR, C-13-NMR and LC-MS. Their biological activities were evaluated against Schistosoma japonicum in mice by an oral route. Among these compounds, in vivo, at concentrations 400mg/kg of mouse, compound 1-(biphenyl-4'-yloxy)-3-(1'-(3',4'-difluorophenyl)ethylamino)propan-2-ol (3j) produced the highest activity with 93.0% deparasitization. These compounds may find usefulness in the discovery and development of new antischistosomal drugs.

• 出版日期2012-9
• 单位中国疾病预防控制中心寄生虫病预防控制所; 中国疾病预防控制中心