28249-75-4Relevant articles and documents
Biological evaluation the 2-aryl-2,3-dihydrobenzodiazaborinin-4(1H)-ones as potential dual α-glucosidase and α-amylase inhibitors with antioxidant properties
Mphahlele, Malose J.,Magwaza, Nontokozo M.,Malindisa, Sibusiso T.,Choong, Yee Siew
, p. 234 - 247 (2021/06/08)
The 2-aryl-2,3-dihydrobenzodiazaborinin-4(1H)-ones (azaborininone) were synthesized as analogues of the 2-arylquinazoline-4-ones and screened through enzymatic assay in vitro for inhibitory effect against α-glucosidase and α-amylase activities. These azaborininones exhibited moderate to good inhibitory effect against these enzymes compared to acarbose used as a reference standard. The results are supported by the enzyme-ligand interactions through kinetics (in vitro) and molecular docking (in silico) studies. The test compounds also exhibited significant antioxidant activity through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) free radical scavenging assays. These azaborininone derivatives exhibited no effect on the viability of the human lung cancer (A549) cell line after 24?hr and were also not toxic towards the Vero cells.
Arynes and Their Precursors from Arylboronic Acids via Catalytic C-H Silylation
Devaraj, Karthik,Ingner, Fredric J.L.,Sollert, Carina,Gates, Paul J.,Orthaber, Andreas,Pilarski, Lukasz T.
, p. 5863 - 5871 (2019/04/16)
A new, operationally simple approach is presented to access arynes and their fluoride-activated precursors based on Ru-catalyzed C-H silylation of arylboronates. Chromatographic purification may be deferred until after aryne capture, rendering the arylboronates de facto precursors. Access to various new arynes and their derivatives is demonstrated, including, for the first time, those based on a 2,3-carbazolyne and 2,3-fluorenyne core, which pave the way for novel derivatizations of motifs relevant to materials chemistry.
Azaborininones: Synthesis and Structural Analysis of a Carbonyl-Containing Class of Azaborines
Davies, Geraint H. M.,Mukhtar, Asma,Saeednia, Borna,Sherafat, Fatemeh,Kelly, Christopher B.,Molander, Gary A.
, p. 5380 - 5390 (2017/05/24)
An approach to access azaborininones (carbonyl-containing, boron-based heterocyclic scaffolds) using simple reagents and conditions from both organotrifluoroborates and boronic acids is described. An inexpensive, common reagent, SiO2, was found to serve as both a fluorophile and desiccant to facilitate the annulation process across three different azaborininone platforms. Computational analysis of some of the cores synthesized in this study was undertaken to compare the azaborininones with the analogous carbon-based heterocyclic systems. Computationally derived pKa values, NICS aromaticity calculations, and electrostatic potential surfaces revealed a unique isoelectronic/isostructural relationship between these azaborines and their carbon isosteres that changed based on boron connectivity. Correlation to experimentally derived data supports the computational findings.