The design, synthesis, and biological evaluation of beta-keto sulfones as 11beta-HSD1 inhibitors and the mechanism of inhibition are described here. This class of compounds is not active against 11beta-HSD2 and therefore may have therapeutic potential for metabolic syndrome and type 2 diabetes.
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http://dx.doi.org/10.1016/j.bmc.2007.04.035 | DOI Listing |
Appl Biochem Biotechnol
January 2025
Department of Chemistry, Late Pushpadevi Patil Arts and Science College, Risod, Dist. Washim, Maharashtra, 444506, India.
We report the first in situ reaction of the β-haloketones obtained from laccase catalysed oxidation of secondary alcohol 2-halo phenylethanol's in present study. To the best of our knowledge, this is the first ever fusion of laccase catalysed oxidation reaction with green organic synthetic reaction. The methodology employs molecular oxygen to oxidize secondary alcohol in biphasic medium by laccase from T.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz - FIOCRUZ, Av. Brasil, 4365, Rio de Janeiro, 21040-900, Brazil. Electronic address:
J Org Chem
October 2024
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China.
A simple and high-yielding strategy to produce a variety of β-keto sulfides using asymmetrical and symmetrical thiosulfonates with ketones under mild conditions is reported. It was found that the various substituted compounds, with both electron-withdrawing and electron-donating substituents, afforded a wide range of β-keto thiosulfones (α-thioaryl-β-keto sulfones) in moderate to high yields. The transformations were reliable at the gram-scale, thus illustrating their efficiency and practicality.
View Article and Find Full Text PDFMolecules
July 2024
School of Chemistry, South China Normal University, Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, GDMPA Key Laboratory for Process Control and Quality Evaluation of Chiral Pharmaceuticals, Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, Guangzhou 510006, China.
An efficient and operationally simple method for the synthesis of β-keto sulfones through the BF·OEt-promoted reaction of alkynes and sodium sulfinates is developed. With its facile and selective access to the targets, it features good functional group compatibility, mild conditions, easily available starting materials, and good yields. Notably, the reaction does not require metal catalysts or chemical reagents with pungent odors.
View Article and Find Full Text PDFJ Org Chem
August 2024
Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi 221005, India.
An efficient visible-light-induced synthesis of vinyl sulfones has been accomplished via decarboxylative sulfonylation of cinnamic acids using sulfonylazides, -toluenesulfonylmethyl isocyanide, and β-keto sulfones as sulfonyl source, in the presence of inexpensive organic photocatalysts like rhodamine B and eosin Y. The reaction is facile, straightforward, and endowed with wide substrate scope and functional group tolerability.
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