Novel Aminoalcohol Derivatives Bearing 4-Phenylphenol as Antischistosomal Drugs
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
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