Literature DB >> 24900723

Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.

Peter M Njogu1, Jiri Gut2, Philip J Rosenthal2, Kelly Chibale3.   

Abstract

A series of hybrid compounds based on (2R,3S)-N-benzoyl-3-phenylisoserine, artemisinin, and quinoline moieties was synthesized and tested for in vitro antiplasmodial activity against erythrocytic stages of K1 and W2 strains of Plasmodium falciparum. Two hybrid compounds incorporating (2R,3S)-N-benzoyl-3-phenylisoserine and artemisinin scaffolds were 3- to 4-fold more active than dihydroartemisinin, with nanomolar IC50 values against Plasmodium falciparum K1 strain.

Entities:  

Keywords:  (2R,3S)-N-Benzoyl-3-phenylisoserine; antiplasmodial activity; artemisinin; hybrids; quinoline

Year:  2013        PMID： 24900723      PMCID： PMC4027494          DOI： 10.1021/ml400164t

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


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