Your browser doesn't support javascript.
loading
3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally.
Leven, Michael; Knaab, Tanja C; Held, Jana; Duffy, Sandra; Meister, Stephan; Fischli, Christoph; Meitzner, Diane; Lehmann, Ursula; Lungerich, Beate; Kuna, Krystina; Stahlke, Petra; Delves, Michael J; Buchholz, Mirko; Winzeler, Elizabeth A; Avery, Vicky M; Mordmüller, Benjamin; Wittlin, Sergio; Kurz, Thomas.
Afiliação
  • Leven M; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf , Universitätsstraße 1, 40225 Düsseldorf, Germany.
  • Knaab TC; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf , Universitätsstraße 1, 40225 Düsseldorf, Germany.
  • Held J; Institut für Tropenmedizin, Eberhard Karls Universität Tübingen , Wilhelmstraße 27, 72074 Tübingen, Germany.
  • Duffy S; Centre de Recherches Medicales de Lambaréné , B.P.: 242 Lambaréné, Gabon.
  • Meister S; Griffith Institute for Drug Discovery, Griffith University , Brisbane Innovation Park, Don Young Road, Nathan, Queensland 4111, Australia.
  • Fischli C; Department of Pediatrics, School of Medicine, University of California, San Diego , La Jolla, California 92093, United States.
  • Meitzner D; Swiss Tropical and Public Health Institute , Socinstraße 57, 4002 Basel, Switzerland.
  • Lehmann U; University of Basel , CH-4003 Basel, Switzerland.
  • Lungerich B; Department of Drug Design and Target Validation, Fraunhofer-Institut für Zelltherapie und Immunologie , Weinbergweg 22, 06120 Halle (Saale), Germany.
  • Kuna K; Swiss Tropical and Public Health Institute , Socinstraße 57, 4002 Basel, Switzerland.
  • Stahlke P; University of Basel , CH-4003 Basel, Switzerland.
  • Delves MJ; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf , Universitätsstraße 1, 40225 Düsseldorf, Germany.
  • Buchholz M; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf , Universitätsstraße 1, 40225 Düsseldorf, Germany.
  • Winzeler EA; Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf , Universitätsstraße 1, 40225 Düsseldorf, Germany.
  • Avery VM; Cell and Molecular Biology, Department of Life Sciences, Imperial College , London SW7 2AZ, U.K.
  • Mordmüller B; Department of Drug Design and Target Validation, Fraunhofer-Institut für Zelltherapie und Immunologie , Weinbergweg 22, 06120 Halle (Saale), Germany.
  • Wittlin S; Department of Pediatrics, School of Medicine, University of California, San Diego , La Jolla, California 92093, United States.
  • Kurz T; Griffith Institute for Drug Discovery, Griffith University , Brisbane Innovation Park, Don Young Road, Nathan, Queensland 4111, Australia.
J Med Chem ; 60(14): 6036-6044, 2017 07 27.
Article em En | MEDLINE | ID: mdl-28653845
ABSTRACT
Structural optimization of 3-hydroxy-N'-arylidenepropanehydrazonamides provided new analogs with nanomolar to subnanomolar antiplasmodial activity against asexual blood stages of Plasmodium falciparum, excellent parasite selectivity, and nanomolar activity against the earliest forms of gametocyte development. Particularly, derivatives with a 1,3-dihalo-6-trifluoromethylphenanthrene moiety showed outstanding in vivo properties and demonstrated in part curative activity in the Plasmodium berghei mouse model when administered perorally.
Assuntos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenantrenos / Plasmodium berghei / Amidas / Hidrazonas / Malária / Antimaláricos Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Alemanha
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenantrenos / Plasmodium berghei / Amidas / Hidrazonas / Malária / Antimaláricos Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Alemanha