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N-acylated sulfonamide congeners of fosmidomycin lack any inhibitory activity against DXR.
Gadakh, Bharat; Pouyez, Jenny; Wouters, Johan; Venkatesham, Akkaladevi; Cos, Paul; Van Aerschot, Arthur.
Afiliación
  • Gadakh B; Medicinal Chemistry, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium.
  • Pouyez J; Department of Chemistry, University of Namur, Rue de Bruxelles 61, Namur B-5000, Belgium.
  • Wouters J; Department of Chemistry, University of Namur, Rue de Bruxelles 61, Namur B-5000, Belgium.
  • Venkatesham A; Medicinal Chemistry, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium.
  • Cos P; Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, Universiteitsplein 1, 2610 Wilrijk, Belgium.
  • Van Aerschot A; Medicinal Chemistry, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium.
Bioorg Med Chem Lett ; 25(7): 1577-9, 2015 Apr 01.
Article en En | MEDLINE | ID: mdl-25726328
ABSTRACT
The antibiotic fosmidomycin (3a) is an inhibitor of the non-mevalonate pathway for isoprenoid biosynthesis. Four analogues in which an acylated sulfonamide group is substituting for its phosphonate moiety have been synthesized in a fruitless effort to preserve one negative charge in order to increase the accompanying affinity for 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), the fosmidomycin target enzyme.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Sulfonamidas / Isomerasas Aldosa-Cetosa / Fosfomicina / Antibacterianos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Bélgica

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Sulfonamidas / Isomerasas Aldosa-Cetosa / Fosfomicina / Antibacterianos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Bélgica