Coordination Assemblies of Acetylenic Dithioether Ligands on Silver(I) Salts: Crystal Structure, Antibacterial and Cytotoxicity Activities.

Coordination polymers (CPs) and metal-organic frameworks (MOFs) constitute a new class of antibacterial materials. Interest in them stems from their wide range of topology, dimensionality, and secondary building units that can be tuned by an appropriate choice of metal ions and ligands. In particular, silver-based species feature good antibacterial properties.

Exploiting π and Chalcogen Interactions for the β-Selective Glycosylation of Indoles through Glycal Conformational Distortion.

Harnessing unconventional noncovalent interactions (NCIs) is emerging as a formidable synthetic approach in difficult-to-access glycosidic chemical space. C-Glycosylation, in particular, has gained a flurry of recent attention. However, most reported methods are restricted to the relatively facile access to α-C-glycosides.

Cooperative Bifurcated Chalcogen Bonding and Hydrogen Bonding as Stereocontrolling Elements for Selective Strain-Release Septanosylation.

The exploitation of noncovalent interactions (NCIs) is emerging as a vital handle in tackling broad stereoselectivity challenges in synthesis. In particular, there has been significant recent interest in the harnessing of unconventional NCIs to surmount difficult selectivity challenges in glycosylations. Herein, we disclose the exploitation of an unconventional bifurcated chalcogen bonding and hydrogen bonding (HB) network, which paves the way for a robust catalytic strategy into biologically useful seven-membered ring sugars.

Synthesis of Tetracyclic Spirooxindolepyrrolidine-Engrafted Hydantoin Scaffolds: Crystallographic Analysis, Molecular Docking Studies and Evaluation of Their Antimicrobial, Anti-Inflammatory and Analgesic Activities.

In a sustained search for novel potential drug candidates with multispectrum therapeutic application, a series of novel spirooxindoles was designed and synthesized via regioselective three-component reaction between isatin derivatives, 2-phenylglycine and diverse arylidene-imidazolidine-2,4-diones (Hydantoins). The suggested stereochemistry was ascertained by an X-ray diffraction study and NMR spectroscopy. The resulting tetracyclic heterocycles were screened for their in vitro in vivo anti-inflammatory and analgesic activity and for their in vitro antimicrobial potency.

Collective Synthesis of Sarpagine and Macroline Alkaloid-Inspired Compounds.

Design strategies that can access natural-product-like chemical space in an efficient manner may facilitate the discovery of biologically relevant compounds. We have employed a divergent intermediate strategy to construct an indole alkaloid-inspired compound collection derived from two different molecular design principles, i.e.

Petasis Sequence Reactions for the Scaffold-Diverse Synthesis of Bioactive Polycyclic Small Molecules.

The multicomponent Petasis reaction is a versatile method to access functionalized amines. The combination of Petasis reaction with subsequent ring-closing reactions is a powerful strategy to build novel polycyclic scaffolds. In this study, we report the generation of a diverse set of small molecules with polycyclic scaffolds featuring a high content of sp-hybridized carbon atoms and multiple stereogenic centers by employing three-component Petasis reaction (3C-PR)-Intramolecular Diels-Alder (IMDA) and 3C-PR-ring-closing metathesis (RCM)-IMDA sequence reactions.

A Silicon-Stereogenic Silanol - O-Isotope Labeling and Stereogenic Probe Reveals Hidden Stereospecific Water Exchange Reaction.

A silicon-stereogenic aminosilanol was isolated in excellent diastereomeric ratio and the absolute configuration was determined. The silanol is configurative and condensation stable in solution and shows stereoselective transformations with a clean stereospecific pathway in follow-up reactions, which leads to the isolation of a silicon-stereogenic zinc complex and siloxane compounds. Investigations with O-labelled water and mass spectrometry analysis revealed an otherwise hidden exchange of oxygen atoms of silanol and water in solution that proceeds with retention of the configuration at the silicon center.

Design of Novel Enantiopure Dispirooxindolopyrrolidine-Piperidones as Promising Candidates toward COVID-19: Asymmetric Synthesis, Crystal Structure and Studies.

Despite the effectiveness of COVID-19 vaccines, there is still an urgent need for discovering new anti-viral drugs to address the awful spread and transmission of the rapidly modifiable virus. In this study, the ability of a small library of enantiomerically pure spirooxindolopyrrolidine-grafted piperidones to inhibit the main protease of SARS-CoV-2 (M) is evaluated. These spiroheterocycles were synthesized by 1,3-dipolar cycloaddition of various stabilized azomethine ylides with chiral dipolarophiles derived from [-(-)-methylbenzyl]-4-piperidone.

Crystal structure and Hirshfeld surface analysis of 1-[(benzyl-dimethyl-sil-yl)meth-yl]-1-ethyl-piperidin-1-ium ethane-sulfonate.

The title mol-ecular salt, CHNSi·CHOS, belongs to the class of -amino-silanes and was synthesized by the alkyl-ation of 1-[(benzyl-dimethyl-sil-yl)meth-yl]piperidine using diethyl sulfate. This achiral salt crystallizes in the chiral space group 2. One of the Si-C bonds in the cation is unusually long [1.

Crystal structure and Hirshfeld surface analysis of ()--methyl-1-phenyl-ethan-1-aminium chloride.

The title compound CHN·Cl, (), can be synthesized starting from ()--methyl-1-phenyl-ethan-1-amine (). Compound upon addition of HCl·EtO leads to crystallization of compound as colorless blocks. The configuration of compound is stable as well as preserved in space group 222.

Primary Amine Functionalization of Alkoxysilanes: Synthesis, Selectivity, and Mechanistic Insights.

We report a highly selective substitution of silicon-bound methoxy groups by primary lithium amides. This unusual reactivity is possible because of the formation of particularly stable lithium methoxide, which compensates for the decreased Si-N bond enthalpy compared to Si-O bonds. In contrast to substitution reactions on halosilanes, highly selective monosubstitutions under mild conditions are possible, even in the presence of further reactive methoxy groups.