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View article: One‐Step Copper‐Assisted Synthesis of α‐(Styrylsulfonyl)amides via SO <sub>2</sub> Incorporation Under Visible Light
One‐Step Copper‐Assisted Synthesis of α‐(Styrylsulfonyl)amides via SO <sub>2</sub> Incorporation Under Visible Light Open
α‐(Styrylsulfonyl)amides and their related ester analogs are an important class of substances that have been widely used as precursors toward bioactive compounds. While most existing methods for the preparation of related compounds include…
View article: Electrochemical One-Step Synthesis of Alkyne Sulfonates and Sulfonamides: Building Blocks for Highly Substituted Alkenes and 1,3-Butadienes
Electrochemical One-Step Synthesis of Alkyne Sulfonates and Sulfonamides: Building Blocks for Highly Substituted Alkenes and 1,3-Butadienes Open
Alkyne motifs have a central place in organic synthesis due to their versatility as building blocks for complex molecule construction. The development of efficient and sustainable strategies for the synthesis of functionalized alkynes rema…
View article: A Short Route to Midazolam via Michael Addition to a Nitroolefin
A Short Route to Midazolam via Michael Addition to a Nitroolefin Open
View article: Surface Density of Mono- and Trivalent High-Mannan-Derived Targeting Structures with Different Affinities Impacts Cellular Uptake of Human Serum Albumin-Derived Nanocarriers
Surface Density of Mono- and Trivalent High-Mannan-Derived Targeting Structures with Different Affinities Impacts Cellular Uptake of Human Serum Albumin-Derived Nanocarriers Open
Actively targeted delivery of nanocarriers (NC) modified with targeting structures (TS) binding to cell surface receptors, specific to target cells, enables enhanced selectivity and efficacy of cellular uptake. This is influenced by the li…
View article: Photoredox‐Catalyzed Synthesis of a Novel Class of Fluoroalkyl Pyrazolones
Photoredox‐Catalyzed Synthesis of a Novel Class of Fluoroalkyl Pyrazolones Open
A photoredox‐enabled strategy is developed for the regioselective synthesis of fluoroalkyl 2‐pyrazolin‐5‐ones via radical addition–cyclization cascades. This metal‐free approach enables the efficient incorporation of perfluoroalkyl and dif…
View article: Inhibitor fluorination pattern tunes chemically induced protein dimerization
Inhibitor fluorination pattern tunes chemically induced protein dimerization Open
Chemically induced dimerization of proteins is a powerful approach to regulate biomolecular functions through small molecule ligands acting as “molecular glues”. Here, we demonstrate that simple, thienopyrimidinone scaffold-based inhibitor…
View article: Biosynthesis of the Paecilomyces marquandii conidial pigment saintopin
Biosynthesis of the Paecilomyces marquandii conidial pigment saintopin Open
View article: Biosynthesis of the Fungal Cyclic Lipodepsipeptide Pleosporacin, a New Selective Inhibitor of the Phytopathogen <i>Botrytis cinerea</i>
Biosynthesis of the Fungal Cyclic Lipodepsipeptide Pleosporacin, a New Selective Inhibitor of the Phytopathogen <i>Botrytis cinerea</i> Open
Bioactivity‐guided isolation led to the identification of the cyclic lipodepsipeptide pleosporacin ( 1 ) from the mycelia extract of fungal strain Pleosporales sp. IBWF 020‐21, a potent selective inhibitor of the fungal phytopathogen Botry…
View article: Allantofuranone Biosynthesis and Precursor-Directed Mutasynthesis of Hydroxylated Analogues
Allantofuranone Biosynthesis and Precursor-Directed Mutasynthesis of Hydroxylated Analogues Open
Genome mining and heterologous reconstitution of biosynthetic genes in Aspergillus oryzae enabled elucidation of the hitherto elusive biosynthetic route that produces allantofuranone (1), a bioactive natural product originall…
View article: Visible Light‐Mediated Diastereoselective Synthesis of Novel Glycopeptide Mimetics
Visible Light‐Mediated Diastereoselective Synthesis of Novel Glycopeptide Mimetics Open
Herein, we introduce a mild and operationally simple visible‐light photochemistry protocol for the synthesis of novel glycopeptide mimetics. This method capitalizes on the reaction between 1,4‐dihydropyridine (DHP) containing amino acids a…
View article: Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus <i>Samsoniella aurantia</i>
Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus <i>Samsoniella aurantia</i> Open
During the course of our studies on the secondary metabolism of rare, hitherto untapped Thai insect-associated fungi, the ethyl acetate (EtOAc) extract derived from solid-state cultivation of Samsoniella aurantia on rice afforded one previ…
View article: Biosynthesis of the Antifungal Polyhydroxy-Polyketide Acrophialocinol
Biosynthesis of the Antifungal Polyhydroxy-Polyketide Acrophialocinol Open
Bioactivity-guided isolation identified the main antifungal compounds produced by Acrophialophora levis as the new polyhydroxy-polyketides acrophialocinol (1) and acrophialocin (2). Their biosynthesis was elucidated by…
View article: Front Cover: Versatile Metal‐Free Arylation of BODIPY and Bis(BF<sub>2</sub>) Chromophores by Using Arylazosulfones in a Sunflow System (Chem. Eur. J. 61/2024)
Front Cover: Versatile Metal‐Free Arylation of BODIPY and Bis(BF<sub>2</sub>) Chromophores by Using Arylazosulfones in a Sunflow System (Chem. Eur. J. 61/2024) Open
View article: Correction: Kommerein et al. Antiplanktonic and Antibiofilm Activity of Rheum palmatum Against Streptococcus oralis and Porphyromonas gingivalis. Microorganisms 2022, 10, 965
Correction: Kommerein et al. Antiplanktonic and Antibiofilm Activity of Rheum palmatum Against Streptococcus oralis and Porphyromonas gingivalis. Microorganisms 2022, 10, 965 Open
In the original publication [...]
View article: Synthesis of 3-substituted pyrrolidin-2-ones and 3-substituted piperidin-2-ones from esters
Synthesis of 3-substituted pyrrolidin-2-ones and 3-substituted piperidin-2-ones from esters Open
View article: Substitution-Induced Mechanistic Switching in SNAr-Warheads for Cysteine Proteases
Substitution-Induced Mechanistic Switching in SNAr-Warheads for Cysteine Proteases Open
The aim of this study was to investigate the transition from non-covalent reversible over covalent reversible to covalent irreversible inhibition of cysteine proteases by making delicate structural changes to the warhead scaffold. To this …
View article: Introducing Targeting Units or pH-Releasable Immunodrugs into Core-Clickable Nanogels
Introducing Targeting Units or pH-Releasable Immunodrugs into Core-Clickable Nanogels Open
The development of nano-sized carrier systems plays a fundamental role in immunodrug delivery and the treatment of cancer. Especially functional materials, coupled with a stimuli-responsive drug release, control the selective delivery of s…
View article: Acremochlorin O and Other Prenylated Chlorophenol Antimicrobial Metabolites from the Fungus <i>Acremonium</i> sp. Strain MNA-F-1
Acremochlorin O and Other Prenylated Chlorophenol Antimicrobial Metabolites from the Fungus <i>Acremonium</i> sp. Strain MNA-F-1 Open
Chemical investigation of the ethyl acetate extract of the fungus Acremonium sp., derived from the inner tissue of anise roots, led to the isolation and characterization of one new chlorinated compound, acremochlorin O ( 1 ), together with…
View article: Solving A Mystery with Classical and Dual Photoredox Catalysis: Application of Nickel in the Synthesis of Ergot Alkaloids
Solving A Mystery with Classical and Dual Photoredox Catalysis: Application of Nickel in the Synthesis of Ergot Alkaloids Open
A short synthesis of the ergot alkaloid lysergene and a formal total synthesis of lysergic acid diethylamide (LSD) under avoidance of palladium and including two nickel-catalyzed steps instead has been developed. A key intermediate of this…
View article: Solving A Mystery with Classical and Dual Photoredox Catalysis: Application of Nickel in the Synthesis of Ergot Alkaloids
Solving A Mystery with Classical and Dual Photoredox Catalysis: Application of Nickel in the Synthesis of Ergot Alkaloids Open
A short synthesis of the ergot alkaloid lysergene and a formal total synthesis of lysergic acid diethylamide (LSD) under avoidance of palladium and including two nickel-catalyzed steps instead has been developed. A key intermediate of this…
View article: Total Synthesis, Structure Reassignment, and Biological Evaluation of the Anti-Inflammatory Macrolactone 13-Hydroxy-14-deoxyoxacyclododecindione
Total Synthesis, Structure Reassignment, and Biological Evaluation of the Anti-Inflammatory Macrolactone 13-Hydroxy-14-deoxyoxacyclododecindione Open
Herein, the first total synthesis of natural 13-hydroxy-14-deoxyoxacyclododecindione along with the revision of the proposed configuration is reported. This natural product, initially discovered in 2018, belongs to the oxacyclododecindione…
View article: P103 14-Deoxy-14-methyloxacyclododecindione: a new therapeutic approach of SLE?
P103 14-Deoxy-14-methyloxacyclododecindione: a new therapeutic approach of SLE? Open
Objective Systemic lupus erythematosus (SLE) is a systemic chronic autoimmune disease characterized by dysregulation of immune system. Increased immune cell activity, impaired phagocytosis as well as formation and deposition of autoantibod…
View article: Acremochlorin S and Other Prenylated Chlorophenol Antimicrobial Metabolites from the Fungus Acremonium Sp. Strain Mna-F-1
Acremochlorin S and Other Prenylated Chlorophenol Antimicrobial Metabolites from the Fungus Acremonium Sp. Strain Mna-F-1 Open
View article: One-Pot Synthesis of Cereblon Proteolysis Targeting Chimeras via Photoinduced C(sp<sup>2</sup>)–C(sp<sup>3</sup>) Cross Coupling and Amide Formation for Proteolysis Targeting Chimera Library Synthesis
One-Pot Synthesis of Cereblon Proteolysis Targeting Chimeras via Photoinduced C(sp<sup>2</sup>)–C(sp<sup>3</sup>) Cross Coupling and Amide Formation for Proteolysis Targeting Chimera Library Synthesis Open
In this study, a one-pot synthesis via photoinduced C(sp2)-C(sp3) coupling followed by amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The described protocol was studied on cereblon (…
View article: NMR and Docking Calculations Reveal Novel Atomistic Selectivity of a Synthetic High-Affinity Free Fatty Acid vs. Free Fatty Acids in Sudlow’s Drug Binding Sites in Human Serum Albumin
NMR and Docking Calculations Reveal Novel Atomistic Selectivity of a Synthetic High-Affinity Free Fatty Acid vs. Free Fatty Acids in Sudlow’s Drug Binding Sites in Human Serum Albumin Open
Saturation transfer difference (STD), inter-ligand NOEs (INPHARMA NMR), and docking calculations are reported for investigating specific binding sites of the high-affinity synthetic 7-nitrobenz-2-oxa-1,3-diazoyl-4-C12 fatty acid (NBD-C12 F…
View article: Two new steroids from the medicinal plant Physalis peruviana L.
Two new steroids from the medicinal plant Physalis peruviana L. Open
View article: Discovery and characterisation of a broderol‐like illudin, omphaderol in the mycelial extracts of <i>Omphalotus mexicanus</i> (Omphalotaceae) using UPLC‐QTOF‐MS and NMR spectroscopy
Discovery and characterisation of a broderol‐like illudin, omphaderol in the mycelial extracts of <i>Omphalotus mexicanus</i> (Omphalotaceae) using UPLC‐QTOF‐MS and NMR spectroscopy Open
Introduction The genus Omphalotus , in particular the “Jack‐O'Lantern mushrooms” Omphalotus illudens and Omphalotus olearius , are famous for the production of the DNA‐alkylating illudins. A lesser‐known species, Omphalotus mexicanus , nat…
View article: CCDC 2209471: Experimental Crystal Structure Determination
CCDC 2209471: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Short and Efficient Synthesis of the Antituberculosis Agent Pretomanid from (<i>R</i>)-Glycidol
Short and Efficient Synthesis of the Antituberculosis Agent Pretomanid from (<i>R</i>)-Glycidol Open
An efficient gram-scale synthesis of the antituberculosis agent pretomanid using straightforward chemistry, mild reaction conditions, and readily available starting materials is reported. Four different protecting groups on the glycidol mo…
View article: One-pot synthesis of CRBN PROTACs via photoinduced C(sp2)–C(sp3) cross coupling and amide formation for PROTAC library synthesis
One-pot synthesis of CRBN PROTACs via photoinduced C(sp2)–C(sp3) cross coupling and amide formation for PROTAC library synthesis Open
In this study, a one-pot synthesis via photoinduced C(sp2)–C(sp3) coupling followed by amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The described protocol was studied on cereblon (CRBN)-based E3-ligase …