Literature DB >> 12699750

Structure-activity relationships of novel anti-malarial agents. Part 6: N-(4-arylpropionylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.

Jochen Wiesner1, Katharina Fucik, Katja Kettler, Jacek Sakowski, Regina Ortmann, Hassan Jomaa, Martin Schlitzer.   

Abstract

We have demonstrated that the p-trifluoromethylphenylpropionylamino residue at the 2-position of the core structure leads to an active benzophenone-type anti-malarial agent. The attempt to improve water solubility by introduction of an amino group into the alpha-position of the arylpropionyl residue resulted in decreased activity.

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Year:  2003        PMID: 12699750     DOI: 10.1016/s0960-894x(03)00179-3

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.

Authors:  Wesley C Van Voorhis; Kasey L Rivas; Pravin Bendale; Laxman Nallan; Carolyn Hornéy; Lynn K Barrett; Kevin D Bauer; Brian P Smart; Sudha Ankala; Oliver Hucke; Christophe L M J Verlinde; Debopam Chakrabarti; Corey Strickland; Kohei Yokoyama; Frederick S Buckner; Andrew D Hamilton; David K Williams; Louis J Lombardo; David Floyd; Michael H Gelb
Journal:  Antimicrob Agents Chemother       Date:  2007-07-02       Impact factor: 5.191

  1 in total

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