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Atroposelective transformation of axially chiral (hetero)biaryls. From desymmetrization to modern resolution strategies
(Royal Society of Chemistry, 2021)
This tutorial review provides a systematic overview of the available methodologies for the atroposelective transformation of (heterobiaryl)biaryl precursors toward the synthesis of enantiomerically enriched products and ...
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Fluoro-labelled sp2-iminoglycolipids with immunomodulatory properties
(Elsevier, 2023)
The unique electronic properties of the fluorine atom make its strategic incorporation into a bioactive compound a very useful tool in the design of drugs with optimized pharmacological properties. In the field of the ...
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Ir-Catalyzed Atroposelective Desymmetrization of Heterobiaryls: Hydroarylation of Vinyl Ethers and Bicycloalkenes
(American Chemical Society, 2020)
A highly regio-, diastereo-, and enantioselective, scalable Ir-catalyzed hydroarylation of electron-rich acyclic and tensioned cyclic olefins with heterobiaryls is described. The reaction of acyclic vinyl ethers, dihydrofuran, ...
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Scope and Limitations of Current Antibiotic Therapies against Helicobacter pylori: Reviewing Amoxicillin Gastroretentive Formulations
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
Even though general improvement of quality of life has happened around the globe, statistics show that gastric cancer is still a very serious medical concern in some regions of the world. A big portion of malignant neoplasms ...
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Conformationally Restricted Glycoconjugates Derived from Arylsulfonamides and Coumarins: New Families of Tumour-Associated Carbonic Anhydrase Inhibitors
(Multidisciplinary Digital Publishing Institute (MDPI), 2023)
The involvement of carbonic anhydrases (CAs) in a myriad of biological events makes the development of new inhibitors of these metalloenzymes a hot topic in current Medicinal Chemistry. In particular, CA IX and XII are ...
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Tacrine-sugar mimetic conjugates as enhanced cholinesterase inhibitors
(Royal Society of Chemistry, 2021-03-14)
We have used the Cu(i)-catalyzed azide-alkyne Huisgen cycloaddition reaction to obtain two families of bivalent heterodimers where tacrine is connected to an azasugar or iminosugar, respectively,vialinkers of variable ...
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Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
(Taylor & Francis Open Access, 2021)
The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters ...
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AuI-Catalyzed Haloalkynylation of Alkenes
(Wiley-Blackwell, 2020)
The formal insertion of alkenes into aromatic chloro- and bromoalkynes takes place under cationic gold catalysis. This haloalkynylation reaction can be performed with cyclic, gem-disubstituted and monosubstituted alkenes, ...
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Discovery of human hexosaminidase inhibitors by in situ screening of a library of mono- and divalent pyrrolidine iminosugars
(Elsevier, 2022)
Two libraries of mono- and dimeric pyrrolidine iminosugars were synthesized by CuAAC and (thio)urea-bond-forming reactions from the respective azido/aminohexylpyrrolidine iminosugar precursors. The resulting monomeric and ...
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Exploring Multi-Subsite Binding Pockets in Proteins: DEEP-STD NMR Fingerprinting and Molecular Dynamics Unveil a Cryptic Subsite at the GM1 Binding Pocket of Cholera Toxin B
(Wiley, 2020)
Ligand-based NMRtechniquesto studyprotein–ligandinteractionsare potenttoolsin drugdesign.Satura-tiontransfer difference (STD)NMRspectroscopystandsoutas one of the mostversatiletechniques,allowing screeningof fragmentslibraries ...