Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Novel Aminoalcohol Derivatives Bearing 4-Phenylphenol as Antischistosomal Drugs

Author(s): 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

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Article Details

VOLUME: 9
ISSUE: 7
Year: 2012
Page: [694 - 697]
Pages: 4
DOI: 10.2174/157018012801319490
Price: $58