Henner Knust
Hoffmann-La Roche
96 Papers
552 Citations
Henner Knust is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Alkyl & Alkoxy group. The author has an hindex of 18, co-authored 96 publications. Previous affiliations of Henner Knust include ETH Zurich & Simon Fraser University.
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Papers
Synthesis and Structural Analysis of a New Class of Azaspiro[3.3]heptanes as Building Blocks for Medicinal Chemistry
TL;DR: These spirocyclic systems may be considered as alternatives to 1,3-heteroatom-substituted cyclohexanes, which are otherwise insufficiently stable to allow their use in drug discovery.
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Direct photocatalytic fluorination of benzylic C–H bonds with N-fluorobenzenesulfonimide
Matthew B. Nodwell,Abhimanyu Bagai,Shira D. Halperin,Rainer E. Martin,Henner Knust,Robert Britton +5 more
TL;DR: Two complimentary strategies for the direct fluorination of benzylic C-H bonds using N-fluorobenzenesulfonimide and either a decatungstate photocatalyst or AIBN-initiation are reported.
103
Identification of Three Novel Radiotracers for Imaging Aggregated Tau in Alzheimer’s Disease with Positron Emission Tomography
Luca Gobbi,Henner Knust,Matthias Körner,Michael Honer,Christian Czech,Sara Belli,Dieter Muri,Martin R. Edelmann,Thomas Hartung,Isabella Erbsmehl,Sandra Grall-Ulsemer,Andreas Koblet,Marianne Rueher,Sandra Steiner,Hayden T. Ravert,William B. Mathews,Daniel P. Holt,Hiroto Kuwabara,Heather Valentine,Robert F. Dannals,Dean F. Wong,Edilio Borroni +21 more
TL;DR: Three novel PET tracers are discovered with high affinity for tau neurofibrillary tangles, excellent selectivity against Aβ plaques, and appropriate pharmacokinetic and metabolic properties in mice and non-human primates.
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Bis(arylvinyl)pyrazines, -pyrimidines, and -pyridazines As Imaging Agents for Tau Fibrils and β-Amyloid Plaques in Alzheimer’s Disease Models
Alexander Boländer,Daniel Kieser,Constantin Voss,Silvia Bauer,Christian Schön,Steffen Burgold,Tobias Bittner,Jana Hölzer,Roland Heyny-von Haußen,Gerhard Mall,Valérie Goetschy,Christian Czech,Henner Knust,Robert Berger,Jochen Herms,Ingrid Hilger,Boris Schmidt +16 more
TL;DR: The synthesis and evaluation of fluorescent pyrazine, pyrimidine, and pyridazine derivatives in vitro and in vivo aiming at a tau-based diagnosis of Alzheimer's disease are reported, finding an AD-related deposition of tau aggregates in the Bowman's glands of the olfactory epithelium, which holds potential for an endoscopic diagnosis of AD in the Olfactory system.
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The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA α5 inverse agonists for the treatment of cognitive dysfunction
Henner Knust,Guido Achermann,Theresa M. Ballard,Bernd Buettelmann,Rodolfo Gasser,Holger Fischer,Maria-Clemencia Hernandez,Frédéric Knoflach,Andreas Koblet,Heinz Stadler,Andrew Thomas,Gerhard Trube,Pius Waldmeier +12 more
TL;DR: The unique pharmacological profiles and optimal pharmacokinetic profiles resulted in in vivo activity in selected cognition models and the identification of two clinical leads functioning as novel potent and selective GABAA alpha5 inverse agonists.
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