Nature research paper: Synthesis of meta-substituted arene bioisosteres from [3.1.1]propellane
-substituted benzene rings in drug design. The utility of these cage structures derives from their superior pharmacokinetic properties compared to the parent aromatics, including improved solubility and reduced susceptibility to metabolism. A prime example is the bicyclo[1.1.1]pentane motif, which is mainly synthesised by ring-opening of the inter-bridgehead bond of the strained hydrocarbon [1.1.
1]heptanes , hydrocarbons whose bridgehead substituents map precisely onto the geometry ofsubstituted benzenes, can be conveniently accessed from [3.1.1]propellane. We found that [3.1.1]propellane can be synthesized on multigram scale, and readily undergoes a range of radical-based transformations to generate medicinally-relevant carbon- and heteroatom-substituted BCHeps, including pharmaceutical analogues.
Ireland Latest News, Ireland Headlines
Similar News:You can also read news stories similar to this one that we have collected from other news sources.
Mostly natural sequencing-by-synthesis for scRNA-seq using Ultima sequencing - Nature BiotechnologyA mostly natural sequencing-by-synthesis method is effective for scRNA-seq, particularly in large-scale studies.
Read more »
CDK11 regulates pre-mRNA splicing by phosphorylation of SF3B1 - NatureCDK11 associates with SF3B1 and phosphorylates threonine residues at the N terminus of SF3B1 during spliceosome activation, and the inhibition of CDK11 blocks the activation and leads to widespread intron retention and the accumulation of non-functional spliceosomes on pre-mRNAs and chromatin.
Read more »
How researchers can join the race to develop new ways of making meat - Nature BiotechnologyThe sustainable protein sector, which promises to create a better food system for the planet, is part of a growing industry with a lot to offer to young researchers.
Read more »
Why paying individual people for their health data is a bad idea - Nature MedicinePaying individual people for their health data will widen inequalities and reduce altruism, luring people to sell their privacy. Health data should instead be treated as collective property, and commercial profits should be shared with the public.
Read more »
Post-infusion CAR TReg cells identify patients resistant to CD19-CAR therapy - Nature MedicineSingle-cell proteomic profiling of circulating CART cells in patients treated with CD19-CAR shows that CD4+Helios+ CAR Treg cells on day 7 after infusion are associated with progressive disease & less severe neurotoxicity in patients with LBCL.
Read more »
Bindi Irwin’s Daughter Grace Has The Cutest Little Walk Exploring Nature in a New Video.BindiIrwin's daughter, Grace, is ready to take on the world with a fierce pep in her step.
Read more »