Lead Optimization Studies on FimH Antagonists: Discovery of Potent and Orally Bioavailable Ortho-substituted Biphenyl Mannosides

Herein, we describe the X-ray structure-based design and optimization of biaryl mannoside FimH inhibitors. Diverse modifications to the biaryl ring to improve drug-like physical and pharmacokinetic properties of mannosides were assessed for FimH binding affinity based on their effects on hemagglutin...

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Библиографические подробности
Главные авторы: Han, Zhenfu, Pinkner, Jerome S., Ford, Bradley, Chorell, Erik, Crowley, Jan M., Cusumano, Corinne K., Campbell, Scott, Henderson, Jeffrey P., Hultgren, Scott J., Janetka, James W.
Формат: Artigo
Язык:Inglês
Опубликовано: 2012
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Article
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC3375398/
https://ncbi.nlm.nih.gov/pubmed/22449031
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300165m
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