In the present study we synthesized new methoxy derivatives of trans 2,3-diaryl-2,3-dihydrobenzofurans, starting from suitable trans 2,3-diaryloxiranes, using regio- and stereoselective nucleophilic oxiranyl ring-opening reactions. The compounds were tested as anti-inflammatories in U937 cells. All compounds showed a significant role in inhibiting the NF-κB pathway and were able to restore normal ROS and NO level upon LPS activation. Moreover, regarding inhibition of ACLY, enantioenriched (50% ee) 7a showed more potency than the racemic counterpart 7arac, together with a higher reduction of prostaglandin E production, thus suggesting a stereoselective interaction in this pathway.
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http://dx.doi.org/10.1016/j.bmcl.2021.128264 | DOI Listing |
AMB Express
January 2025
Faculty of Basic Sciences, King Salman International University, South Sinai City, 46612, Egypt.
The rise of antimicrobial-resistant microorganisms (AMR) poses a significant global challenge to human health and economic stability. In response, various scientific communities are seeking safe alternatives to antibiotics. This study comprehensively investigates the antibacterial effects of red dye derived from Monascus purpureus against three bacterial pathogens: Salmonella typhimurium ATCC14028, Escherichia coli ATCC8739, and Enterococcus faecalis ATCC25923.
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January 2025
Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
In this study, new cinnamic acid linked to triazole acetamide derivatives was synthesized and evaluated for anti-Alzheimer and anti-melanogenesis activities. The structural elucidation of all analogs was performed using different analytical techniques, including H-NMR, C-NMR, mass spectrometry, and IR spectroscopy. The synthesized compounds were assessed in vitro for their inhibitory activities against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase enzymes.
View Article and Find Full Text PDFDalton Trans
January 2025
Laboratory for Molecular & Functional Design, Department of Engineering, Nara Women's University, Nara 630-8506, Japan.
Rational molecular design afforded fluorescent Cd sensors based on bisquinoline derivatives. Introduction of three methoxy groups at the 5,6,7-positions of the quinoline rings of BQDMEN (,'-bis(2-quinolylmethyl)-,'-dimethylethylenediamine) resulted in the reversal of metal ion selectivity in fluorescence enhancement from zinc to cadmium. Introduction of bulky alkyl groups and an ,-bis(2-quinolylmethyl)amine structure, as well as replacement of one of the two tertiary amine binding sites with an oxygen atom and the use of a 1,2-phenylene backbone significantly improved the Cd specificity.
View Article and Find Full Text PDFJ Org Chem
January 2025
Centre for Organometallic Chemistry, School of Chemistry, Bharathidasan University, Tiruchirappalli 620 024, India.
A streamlined strategy for the one-pot synthesis of isoxazolone analogues has been developed through an acceptorless dehydrogenative annulation (ADA) pathway by employing new Ru(II) hydride complexes as effective catalysts. New Ru(II) complexes () tailored with N̂O chelating carbazolone benzhydrazone ligands were synthesized and their formation was confirmed using analytical and spectral techniques including FT-IR and NMR. The structural configuration of the complexes featuring an octahedral geometry around the Ru(II) ion was precisely determined by single-crystal X-ray diffraction analysis.
View Article and Find Full Text PDFEur J Med Chem
December 2024
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, India. Electronic address:
This study presents a comprehensive exploration of the synthesis of novel compounds targeting Chagas Disease (CD) caused by Trypanosoma cruzi. It is a global health threat with over 6-7 million infections worldwide. Addressing challenges in current treatments, the investigation explores diverse compound classes, including thiazoles, thiazolidinone, imidazole, pyrazole, 1,6-diphenyl-1H-pyrazolo[3,4-b] pyridine, pyrrole, naphthoquinone, neolignan, benzeneacyl hydrazones, and chalcones-based compounds.
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