A5010534692- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Click Chemistry and Applications
- Carbohydrate Chemistry and Synthesis
- Glycosylation and Glycoproteins Research
- Chemical synthesis and alkaloids
- Microbial Natural Products and Biosynthesis
- Alzheimer's disease research and treatments
- Parkinson's Disease Mechanisms and Treatments
- Bacterial biofilms and quorum sensing
- Multicomponent Synthesis of Heterocycles
- Catalytic Cross-Coupling Reactions
- Metabolomics and Mass Spectrometry Studies
- Synthesis and biological activity
- Crystallization and Solubility Studies
- Protein Degradation and Inhibitors
- X-ray Diffraction in Crystallography
- Photosynthetic Processes and Mechanisms
- Green IT and Sustainability
- Crystal structures of chemical compounds
- Organic and Inorganic Chemical Reactions
- Antimicrobial Peptides and Activities
- Metal complexes synthesis and properties
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Biological Activity
Umeå University
2006-2019
University Hospital of Umeå
2019
Max Planck Society
2015
Abstract Bioactive compound design based on natural product (NP) structure may be limited because of partial coverage NP‐like chemical space and biological target space. These limitations can overcome by combining NP‐centered strategies with fragment‐based through combination NP‐derived fragments to afford structurally unprecedented “pseudo‐natural products” (pseudo‐NPs). The design, synthesis, evaluation a collection indomorphan pseudo‐NPs that combine biosynthetically unrelated indole‐...
Small organic molecules that inhibit functional bacterial amyloid fibers, curli, are promising new antibiotics. Here we investigated the mechanism by which ring-fused 2-pyridone FN075 inhibits fibrillation of curli protein CsgA. Using a variety biophysical techniques, found promotes CsgA to form off-pathway, non-amyloidogenic oligomeric species. In light generic properties amyloids, tested whether would also affect reaction human α-synuclein, an amyloid-forming involved in Parkinson's...
Abstract Bioactive compound design based on natural product (NP) structure may be limited because of partial coverage NP‐like chemical space and biological target space. These limitations can overcome by combining NP‐centered strategies with fragment‐based through combination NP‐derived fragments to afford structurally unprecedented “pseudo‐natural products” (pseudo‐NPs). The design, synthesis, evaluation a collection indomorphan pseudo‐NPs that combine biosynthetically unrelated indole‐...
ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXTSynthesis of a Novel Tricyclic Peptidomimetic ScaffoldMagnus Sellstedt and Fredrik Almqvist*View Author Information Department Chemistry, Umeå University, SE-901 87 Umeå, Sweden[email protected]Cite this: Org. Lett. 2008, 10, 18, 4005–4007Publication Date (Web):August 15, 2008Publication History Received3 July 2008Published online15 August inissue 18 September...
Abstract A series of compounds based on a novel fluorescent scaffold have been synthesized. Most the displayed high quantum yields fluorescence and unusually long lifetimes. HeLa cells were treated with one its use as dye was demonstrated confocal microscopy.
A novel heterocyclic scaffold with a peptidomimetic backbone structure has been synthesized. The is formed by insertion of primary amines into cyclic sulfone to give the corresponding ring-expanded sulfonamides. By varying amine component, series potentially biologically interesting compounds
A three-component reaction forming dihydro 2,7-naphthyridine-1-ones has been developed. These unstable intermediates can be either oxidized or reduced to form naphthyridones tetrahydro naphthyridones, respectively. The tolerates a large variety of aldehydes and amines, the produced compounds are analogs natural product lophocladine A.
Finding a new drug candidate for selected target is an expensive and time-consuming process. Target guided-synthesis, or in situ click chemistry, concept where the used to template formation of its own inhibitors from reactive building blocks. This could simplify identification candidates. However, with exception one example RNA-target, target-guided synthesis has always employed purified targets. limits number targets that can be screened by method. By applying methods field metabolomics,...
Asymmetric trienamine catalysis was used to synthesize cytochalasin B-like compounds and inhibition of glucose uptake in cancer cells demonstrated.
A variety of ring-fused 2-pyridone-based central fragments were prepared using a strategy inspired by diversity-oriented synthesis. The produced compounds are diverse, yet focused, analogs biologically active peptidomimetic 2-pyridones.
Abstract A four‐component reaction between formyl‐substituted 2‐pyridones, aldehydes, amines, and activated alkenes has been developed. The resulting products are ring‐fused natural‐product‐like isoquinuclidines. Three carbon–carbon bonds, two carbon–nitrogen four or five stereocentres formed in the with overall product yields range 23–67 %. In most cases a single diastereomer was obtained. An intramolecular version of yielded analogues multi‐ring‐fused natural catharanthine step.
An emerging method to help elucidate the mode of action experimental drugs is use untargeted metabolomics cell-systems. The interpretations such screens are however complex and more examples with inhibitors known targets needed. Here two T-cell lines were treated an inhibitor aspartate aminotransferase analyzed GC-MS. interpretation data was enhanced by different cell-lines supports as a target. In addition, suggest unexpected off-target effect on glutamate decarboxylase. results exemplify...
Fluorescent multi-ring-fused 2-pyridones, with chemical resemblance to other biologically active 2-pyridone systems, were solubilized in spherical micelles formed by the ganglioside G(M1) and studied respect their spatial localization rotational mobility. For this, electronic energy transfer between (donor) BODIPY-FL-labeled was determined, as well fluorescence depolarization. From obtained efficiency of acceptor group (BODIPY-FL), either localized polar or nonpolar part ganglioside, it has...
Abstract Coupling of 2‐pyridones with aldehydes, amines, and activated alkenes is found to allow access pharmacologically interesting ring‐fused isoquinuclidines.
ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access Abstract of an article which published elsewhere, please select "Full Text" option. The original trackable via the "References"
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 200 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”