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Eine große Bibliothek von fluorierten Fragmenten wurde synthetisiert, mit dem Ziel eines besseren Samplings des chemischen Raumes und einer einfacheren Screening‐Prozedur. Die Einbeziehung von Fluor ermöglichte ein effizientes Screening mittels 19F‐NMR‐Spektroskopie, was in einem Screening gegen vier krankheitsrelevante Targets demonstriert wurde, das eine Reihe von Startpunkten für die Leitstrukturentwicklung...
Fragment‐based drug discovery (FBDD) is a popular method in academia and the pharmaceutical industry for the discovery of early lead candidates. Despite its wide‐spread use, the approach still suffers from laborious screening workflows and a limited diversity in the fragments applied. Presented here is the design, synthesis, and biological evaluation of the first fragment library specifically tailored...
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