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Synthetic Fosmidomycin analogues with altered chelating moieties do not inhibit 1-deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum growth in vitro.
Chofor, René; Risseeuw, Martijn D P; Pouyez, Jenny; Johny, Chinchu; Wouters, Johan; Dowd, Cynthia S; Couch, Robin D; Van Calenbergh, Serge.
Afiliação
  • Chofor R; Laboratory for Medicinal Chemistry, Ghent University, Harelbekestraat 72, Ghent B-9000, Belgium. rene.chofor@ugent.be.
  • Risseeuw MD; Laboratory for Medicinal Chemistry, Ghent University, Harelbekestraat 72, Ghent B-9000, Belgium. martijn.risseeuw@ugent.be.
  • Pouyez J; Department of Chemistry, University of Namur, UNamur, Rue de Bruxelles 61, Namur B-5000, Belgium. jenny.pouyez@unamur.be.
  • Johny C; Department of Chemistry and Biochemistry, George Mason University, Manassas, VA 20110, USA. cjohny@gmu.edu.
  • Wouters J; Department of Chemistry, University of Namur, UNamur, Rue de Bruxelles 61, Namur B-5000, Belgium. johan.wouters@unamur.be.
  • Dowd CS; Department of Chemistry, George Washington University, Washington, DC 20052, USA. cdowd@gwu.edu.
  • Couch RD; Department of Chemistry and Biochemistry, George Mason University, Manassas, VA 20110, USA. rcouch@gmu.edu.
  • Van Calenbergh S; Laboratory for Medicinal Chemistry, Ghent University, Harelbekestraat 72, Ghent B-9000, Belgium. serge.vancalenbergh@ugent.be.
Molecules ; 19(2): 2571-87, 2014 Feb 24.
Article em En | MEDLINE | ID: mdl-24566322
ABSTRACT
Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. This study further underlines the importance of the hydroxamate functionality and illustrates that identifying effective alternative bidentate ligands for this target enzyme is challenging.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Inibidores Enzimáticos / Eritrócitos / Fosfomicina Limite: Humans Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Bélgica

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Inibidores Enzimáticos / Eritrócitos / Fosfomicina Limite: Humans Idioma: En Revista: Molecules Assunto da revista: BIOLOGIA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Bélgica