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The Intramolecular Povarov Tool in the Construction of Fused Nitrogen-Containing Heterocycles
(Springer, 2023-06)
Nitrogen heterocycles are part of the structure of natural products and agents with
important biological activity, such as antiviral, antibiotic, and antitumor drugs. For
this reason, heterocyclic compounds are one of ...
Lacking Immunotherapy Biomarkers for Biliary Tract Cancer: A Comprehensive Systematic Literature Review and Meta-Analysis
(MDPI, 2023-08-19)
Background: Immunotherapy has recently been incorporated into the spectrum of biliary tract cancer (BTC) treatment. The identification of predictive response biomarkers is essential in order to identify those patients who ...
Synthesis and Characterization of a New Series of Bis(allylic-α-aminophosphonates) under Mild Reaction Conditions
(MDPI, 2023-06-09)
Several bis(α-aminophosphonates) have been conveniently prepared in good yields using a straightforward multicomponent Kabachnik–Fields reaction between ethane 1,2-diamine or propane 1,3-diamine, diethylphosphite and ...
Synthesis of Aminoalkyl Sclareolide Derivatives and Antifungal Activity Studies
(MDPI, 2023-05-12)
Sclareolide was developed as an efficient C-nucleophilic reagent for an asymmetric Mannich addition reaction with a series of N-tert-butylsulfinyl aldimines. The Mannich reaction was carried out under mild conditions, ...
Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions
(MDPI, 2023-01-03)
New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with increased lipophilicity, showed improved efficiency against ...
Gel-Free Tools for Quick and Simple Screening of Anti-Topoisomerase 1 Compounds
(MDPI, 2023-04-27)
With the increasing need for effective compounds against cancer or pathogen-borne diseases, the development of new tools to investigate the enzymatic activity of biomarkers is necessary. Among these biomarkers are DNA ...
Synthesis of 1,2-diaminotruxinic δ-cyclobutanes by BF3-controlled [2 + 2]-photocycloaddition of 5(4H)-oxazolones and stereoselective expansion of δ-cyclobutanes to give highly substituted pyrrolidine-2,5-dicarboxylates
(Royal Society of Chemistry, 2023-04)
The irradiation of (Z)-4-arylidene-5(4H)-oxazolones 1a–1u with blue light (465 nm) in the presence of the photosensitizer [Ru(bpy)3](BF4)2 (2.5 mol%) and the Lewis acid BF3·OEt2 (2 equiv.) in deoxygenated methanol at room ...
New Approved Drugs Appearing in the Pharmaceutical Market in 2022 Featuring Fragments of Tailor-Made Amino Acids and Fluorine
(MDPI, 2023-04-22)
The strategic fluorination of oxidatively vulnerable sites in bioactive compounds is a relatively recent, widely used approach allowing us to modulate the stability, bio-absorption, and overall efficiency of pharmaceutical ...
Enhancing Dual-State Emission in Maleimide Fluorophores through Fluorocarbon Functionalisation
(Wiley, 2022-10)
Herein, a library of trifluoroethyl substituted aminomaleimide derivatives are reported with small size and enhanced emissions in both solution and solid-state. A diCH2CF3 substituted aminochloromaleimide exhibits the most ...
Ba+2 ion trapping using organic submonolayer for ultra-low background neutrinoless double beta detector
(Nature, 2022-12)
If neutrinos are their own antiparticles the otherwise-forbidden nuclear reaction known as neutrinoless double beta decay can occur. The very long lifetime expected for these exceptional events makes its detection a daunting ...