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Synthesis and Evaluation of Quinazolines as Inhibitors of the Bacterial Cell Division Protein FtsZ.
Nepomuceno, Gabriella M; Chan, Katie M; Huynh, Valerie; Martin, Kevin S; Moore, Jared T; O'Brien, Terrence E; Pollo, Luiz A E; Sarabia, Francisco J; Tadeus, Clarissa; Yao, Zi; Anderson, David E; Ames, James B; Shaw, Jared T.
Afiliación
  • Nepomuceno GM; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Chan KM; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Huynh V; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Martin KS; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Moore JT; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • O'Brien TE; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Pollo LA; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Sarabia FJ; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Tadeus C; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Yao Z; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Anderson DE; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Ames JB; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
  • Shaw JT; University of California, Davis , One Shields Avenue, Davis, California 95616, United States.
ACS Med Chem Lett ; 6(3): 308-12, 2015 Mar 12.
Article en En | MEDLINE | ID: mdl-25815151
The bacterial cell division protein FtsZ is one of many potential targets for the development of novel antibiotics. Recently, zantrin Z3 was shown to be a cross-species inhibitor of FtsZ; however, its specific interactions with the protein are still unknown. Herein we report the synthesis of analogues that contain a more tractable core structure and an analogue with single-digit micromolar inhibition of FtsZ's GTPase activity, which represents the most potent inhibitor of Escherichia coli FtsZ reported to date. In addition, the zantrin Z3 core has been converted to two potential photo-cross-linking reagents for proteomic studies that could shed light on the molecular interactions between FtsZ and molecules related to zantrin Z3.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos