Novel Aminoalcohol Derivatives Bearing 4-Phenylphenol as Antischistosomal Drugs

Li-Ping      Duan; Jian      Xue; Yi      Tao; Hao-Bing      Zhang

Abstract

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, 1H-NMR, 13C-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.

Keywords: Aminoalcohol, 4-phenylphenol, Schistosoma japonicum, Drug, antischistosomal, novel aminoalcohol, 13C-NMR, LC-MS, Schistosoma japonicum, therapeutic agents, deparasitization, praziquantel, arylaminoalcohol, 4-phenylphenol scaffold