Your browser doesn't support javascript.
loading
Structure-activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors.
Tran, Tuan P; Ellsworth, Edmund L; Sanchez, Joseph P; Watson, Brian M; Stier, Michael A; Showalter, H D Hollis; Domagala, John M; Shapiro, Martin A; Joannides, E Themis; Gracheck, Stephen J; Nguyen, Dai Q; Bird, Paul; Yip, Judy; Sharadendu, Anurag; Ha, Chan; Ramezani, Saeed; Wu, Xiujuan; Singh, Rajeshwar.
Afiliación
  • Tran TP; Department of Chemistry, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. tuan.tran@pfizer.com
Bioorg Med Chem Lett ; 17(5): 1312-20, 2007 Mar 01.
Article en En | MEDLINE | ID: mdl-17196390
A series of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the optimal substitutions were combined to give two compounds, 2r and 2s, with exceptional enzyme potency (IC50 = 0.2 microM) and activity against gram-positive organisms (MIC's = 0.015-0.06 microg/mL).
Asunto(s)
Buscar en Google
Añadir a Mi BVS
Imprimir
XML
PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinazolinonas / Inhibidores de Topoisomerasa II / Antibacterianos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Buscar en Google
Añadir a Mi BVS
Imprimir
XML
PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinazolinonas / Inhibidores de Topoisomerasa II / Antibacterianos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido