98%
921
2 minutes
20
The synthesis of deflazacort (DFZ) and a preliminary evaluation of its microbial activity against the human pathogens and is herein reported. While DFZ is inactive, one of its synthetic precursors showed a strong antibacterial activity against both Gram-negative and -positive bacteria.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9066171 | PMC |
http://dx.doi.org/10.1039/c9ra03673c | DOI Listing |
J Am Chem Soc
September 2025
Shenzhen Grubbs Institute, Department of Chemistry, Southern University of Science and Technology, Shenzhen 518055, China.
Bicyclo[1.1.1]pentanes (BCPs) play crucial roles as saturated bioisosteric replacements of planar benzene rings.
View Article and Find Full Text PDFOrg Lett
August 2025
Jiangsu Co-Innovation Center for Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, China.
A protocol for the efficient and expeditious synthesis of the pentacyclic C2-spiropseudoindoxyl scaffold that relies on a copper(I)-catalyzed cycloaddition/internal redox (IR)/anthranil formation/oxaziridine formation/ring-opening spirocyclization/reduction cascade of 1-indole -tethered -alkynylnitroarenes is described.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
August 2025
Department of Chemistry and Biochemistry, University of Texas at Dallas, 800 W. Campbell Road, Richardson, TX, 75080, USA.
Methods for introducing subtle modifications at the level of single atoms/bonds ("skeletal editing") are highly desirable in organic and medicinal chemistry, owing to their potential for fine-tuning the structure and biological activity of organic molecules. Here, we report a chemoenzymatic strategy for enabling the skeletal editing of organic frameworks via ring expansion at the level of one or more aliphatic (methylene) C─H sites, as achieved through the synergistic combination of P450-mediated site-selective oxidation with subsequent Baeyer-Villiger rearrangement or ketone homologation. Combining this approach with engineered P450 catalysts exhibiting divergent regioselectivity enabled the expeditious synthesis of a panel of ring-expanded analogs of various complex natural product substrates.
View Article and Find Full Text PDFJ Am Chem Soc
August 2025
Department of Chemistry, University of California, Berkeley, California 94720, United States.
In the past decade, thousands of synthetic building blocks, intermediates, and drug candidates containing a spirocyclopropane core with at least one nitrogen atom have been investigated for a range of biological activities. These compounds create three-dimensional architectures that maintain the rigidity of their more sp-rich analogs. Most examples contain simple core structures with unsubstituted cyclopropyl moieties, and only one has been made enantioselectively.
View Article and Find Full Text PDFChem Commun (Camb)
August 2025
Department of Chemistry, IISER Bhopal, Bhopal Bypass Road, Bhopal - 462 066, Madhya Pradesh, India.
Calycanthaceae alkaloids feature two neighboring carbon atoms that are central to their structure (quaternary stereocenters) and a long, flexible bond between them [elongated labile C3a-C3a's bond] with impressive biological activities. Herein, we envisioned an expeditious approach to dimeric hexahydropyrrolo[2,3]-indoline an unprecedented catalytic asymmetric sequential allylation of ,'-alloc 3,3'-dimeric 2-oxindoles with eventual total syntheses of naturally occurring (-)-calycanthidine and a formal total synthesis of (-)-idiospermuline.
View Article and Find Full Text PDF