Concept
Structure–activity relationship
Publications associées (20)
Oxidation processes and me
This publication summarizes my journey in the field of chemical oxidation processes for water treatment over the last 30+ years. Initially, the efficiency of the application of chemical oxidants for micropollutant abatement was assessed by the abatement of ...
Pergamon-Elsevier Science Ltd2024A multi-reservoir extruder for time-resolved serial protein crystallography and compound screening at X-ray free-electron lasers
Christoph Bostedt, Camila Bacellar Cases Da Silveira
Serial crystallography at X-ray free-electron lasers (XFELs) permits the determination of radiation-damage free static as well as time-resolved protein structures at room temperature. Efficient sample delivery is a key factor for such experiments. Here, we ...
Berlin2023Hypervalent Iodine: New Reagents and Functionalization of Peptides
Alkynes are found in a multitude of natural or synthetic bioactive compounds. In addition to the capacity of these chemical motifs to impact the physicochemical properties of a molecule of interest, the well-established reactivity of alkynes makes them ...
Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries
Christian Heinis, Gerardo Turcatti, Julien Bortoli Chapalay, Alessandro Angelini, Alessandro Zorzi, Jonathan Patrice Vesin, Ganesh Kumar Mothukuri, Sangram Shivdas Kale, Carl Leonard Stenbratt
Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three ...
2020Asymmetric Alkenyl C−H Functionalization by Cp x Rh III forms 2 H ‐Pyrrol‐2‐ones through [4+1]‐Annulation of Acryl Amides and Allenes
Nicolai Cramer, Yang Liu, Shouguo Wang
An efficient CpxRhIII‐catalyzed enantioselective alkenyl C−H functionalization/[4+1] annulation of acryl amides and allenes is reported. The described transformation provides straightforward access to enantioenriched α,β‐unsaturated‐γ‐lactams bearing a qua ...
2019Allosteric cross-talk in chromatin can mediate drug-drug synergy
Paul Joseph Dyson, Ursula Röthlisberger, Tina Riedel, Giulia Palermo
Exploitation of drug-drug synergism and allostery could yield superior therapies by capitalizing on the immensely diverse, but highly specific, potential associated with the biological macromolecular landscape. Here we describe a drug-drug synergy mediated ...
2017Mechanistic Studies on the Stereoselectivity of the Serotonin 5-HT1A Receptor
G-protein-coupled receptors (GPCRs) are involved in a wide range of physiological processes, and they have attracted considerable attention as important targets for developing new medicines. A central and largely unresolved question in drug discovery, whic ...
Wiley-Blackwell2016Intramolecular palladium-catalyzed alkene carboalkynylation
Jérôme Waser, Stefano Nicolai, Peter Swallow
Carbocycles are essential building blocks for the synthesis of natural and synthetic bioactive compounds. Herein, we report the first example of palladium-catalyzed intramolecular carboalkynylation of non-activated olefins. Using activated carbonyl compoun ...
Elsevier2015