A5002395814- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Peptidase Inhibition and Analysis
- Asymmetric Hydrogenation and Catalysis
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Blood Coagulation and Thrombosis Mechanisms
- Catalytic Alkyne Reactions
- Cell Adhesion Molecules Research
- Organoboron and organosilicon chemistry
- Asymmetric Synthesis and Catalysis
- Advanced Synthetic Organic Chemistry
- Inorganic Chemistry and Materials
- RNA and protein synthesis mechanisms
- Hydrogen Storage and Materials
- Oxidative Organic Chemistry Reactions
- Bacterial Genetics and Biotechnology
- Synthesis and Catalytic Reactions
- Marine Sponges and Natural Products
- Fuel Cells and Related Materials
- Phosphodiesterase function and regulation
- Synthesis of β-Lactam Compounds
- Biochemical and Structural Characterization
- Computational Drug Discovery Methods
- Monoclonal and Polyclonal Antibodies Research
- Corporate Governance and Management
AbbVie (Germany)
2013-2020
Abbott (United States)
2013
Abbott (Germany)
2005-2011
BASF (Germany)
1999-2005
Kiel University
2000-2004
Robert Bosch (Germany)
1999
IIT@MIT
1996-1998
Massachusetts Institute of Technology
1996-1998
Technische Universität Berlin
1995-1996
University of Strathclyde
1995-1996
ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTHighly Enantioselective Imine Hydrosilylation Using (S,S)-Ethylenebis(η5-tetrahydroindenyl)titanium DifluorideXavier Verdaguer, Udo E. W. Lange, Matthew T. Reding, and Stephen L. BuchwaldView Author Information Department of Chemistry Massachusetts Institute Technology Cambridge, 02139 Cite this: J. Am. Chem. Soc. 1996, 118, 28, 6784–6785Publication Date (Web):July 17, 1996Publication History Received12 March 1996Published online17 July...
Slow addition of a primary amine to the reaction mixture greatly increases scope titanium-catalyzed asymmetric reduction imines 1. An important added feature this method is that chiral secondary amines 2 can be obtained in much higher optical purity (up 99 % ee) than would predicted from E:Z ratios starting
Multiple technologies have emerged for structural diversification and efficient production of metabolites drug molecules. These include expanded use enzymatic bioorganic transformations that mimic biological systems, biomimetic catalysis electrochemical techniques. As this field continues to mature the breadth is growing beyond simple oxidative processes due in part parallel development more catalytic methods functionalization unactivated scaffolds. allow both aromatic aliphatic substrates...
The efflux transporter P-glycoprotein (P-gp) is responsible for the extrusion of a wide variety molecules, including drug from cell. Therefore, P-gp-mediated transport limits bioavailability drugs. To identify potential P-gp substrates early in discovery process, silico models have been developed based on structural and physicochemical descriptors. In this study, we investigate use molecular dynamics fingerprints (MDFPs) as an orthogonal descriptor training machine learning (ML) to classify...
Summary We have addressed the question whether TFS, a protein that stimulates intrinsic cleavage activity of archaeal RNA polymerase, is able to improve fidelity transcription in Methanococcus . Using non‐specific experiments, we could demonstrate misincorporation non‐templated nucleotides reduced presence TFS. A more detailed analysis revealed elongation complexes containing misincorporated nucleotide were arrested, but be reactivated by RNase as well exonuclease III footprinting...
The development of glycine transporter 1 (GlyT1) inhibitors may offer putative treatments for schizophrenia and other disorders associated with hypofunction the glutaminergic N-methyl-d-aspartate (NMDA) receptor. Herein, we describe synthesis biological evaluation a series 3,4-disubstituted pyrrolidine sulfonamides as competitive GlyT1 that arose from de novo scaffold design. Relationship chemical structure to drug-drug interaction (DDI) bioactivation was mechanistically investigated. Murine...
Durch die langsame Zugabe primärer Amine zur Reaktionsmischung wird Anwendungsbreite der titankatalysierten asymmetrischen Reduktion von Iminen 1 deutlich erweitert. Bemerkenswerterweise liefert diese Methode chirale sekundäre 2 in einer viel höheren optischen Reinheit (bis zu 99% ee), als man aufgrund (E):(Z)-Verhältnisse Iminsubstrate erwarten würde.
The glycine transporter 1 (GlyT1) has emerged as a key novel target for the treatment of schizophrenia. Herein, we report synthesis and biological evaluation aminotetralines aminochromanes classes competitive GlyT1 inhibitors. Starting from high-throughput screening hit, structure–activity relationship studies led first to discovery displaying high potency selectivity, with favorable pharmacokinetic properties. Systematic investigations various parameters (e.g., topological polar surface...
A total synthesis of the sesquiterpene, (+)-taylorione 1 starting from (+)-2-carene is described; key synthetic transformation achieved in high yield by application developed Pauson–Khand reaction techniques for gaseous olefins.
Late-stage functionalization of lead compounds is high interest in drug discovery since it offers an easy access to metabolites and derivatives a compound without the need redesign often long multistep synthesis. Owing their degree chemoselectivity, biocatalytic transformations, enzymatic oxidations particular, are potentially very powerful because they could allow synthesis less lipophilic compound. In majority cases, have been used empirical way as regioselectivity difficult predict. this...
Une étude ethnobotanique auprès des principaux groupes ethniques a été conduite sur les plantes ligneuses dans terroirs riverains de la Réserve biosphère du Mono au Bénin récemment créée et reconnue par l’Unesco en juin 2017. L’objectif cette est déterminer espèces à fortes valeurs d’usage vue mettre disposition gestionnaires importantes conserver promouvoir l’aménagement réserve. Des enquêtes ethnobotaniques ont menées 26 villages réserve où 593 personnes appartenant cinq socio-culturels...