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Fragment-guided design of subnanomolar β-lactamase inhibitors active in vivo

Fragment-based design was used to guide derivatization of a lead series of β-lactamase inhibitors that had heretofore resisted optimization for in vivo activity. X-ray structures of fragments overlaid with the lead suggested new, unanticipated functionality and points of attachment. Synthesis of thr...

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Detalhes bibliográficos
Main Authors: Eidam, Oliv, Romagnoli, Chiara, Dalmasso, Guillaume, Barelier, Sarah, Caselli, Emilia, Bonnet, Richard, Shoichet, Brian K., Prati, Fabio
Formato: Artigo
Idioma:Inglês
Publicado em: National Academy of Sciences 2012
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3491531/
https://ncbi.nlm.nih.gov/pubmed/23043117
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1208337109
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