Synthesis of heterocyclic ring-fused analogs of HMG499 as novel degraders of HMG-CoA reductase that lower cholesterol.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114323
Abstract: HMG-CoA reductase (HMGCR) is the rate-limiting enzyme in cholesterol de novo biosynthesis and its degradation may bring therapeutic benefits for the treatment of cardiovascular disease (CVD) and nonalcoholic steatohepatitis (NASH). Before, we disclosed compound HMG499… read more here.
Keywords: heterocyclic ring; fused analogs; cholesterol; ring fused ... See more keywords
Polysubstituted and ring-fused pyridazine systems from tetrafluoropyridazine
Sign Up to like & getrecommendations! Published in 2017 at "Tetrahedron"
DOI: 10.1016/j.tet.2016.12.006
Abstract: Tetrafluoropyridazine 1 reacts with a range of oxygen-, nitrogen-, sulfur- and carbon-centred nucleophiles to give, in general, products 2 arising from substitution of fluorine para to ring nitrogen. Subsequent reaction of the trifluoropyridazine derivatives 2… read more here.
Keywords: ring fused; fused pyridazine; polysubstituted ring; pyridazine systems ... See more keywords
Ring-Fused Firefly Luciferins: Expanded Palette of Near-Infrared Emitting Bioluminescent Substrates.
Sign Up to like & getrecommendations! Published in 2020 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.9b04562
Abstract: Firefly bioluminescence is broadly applied as a non-invasive imaging modality in the biomedical research field. One limitation in firefly bioluminescence imaging is the limited variety of luciferins emitting in the near-infrared (NIR) region (650-900 nm),… read more here.
Keywords: firefly; ring fused; firefly luciferins; near infrared ... See more keywords
Metal-Free Sequential C(sp2)-H/OH and C(sp3)-H Aminations of Nitrosoarenes and N-Heterocycles to Ring-Fused Imidazoles.
Sign Up to like & getrecommendations! Published in 2017 at "Organic letters"
DOI: 10.1021/acs.orglett.7b00832
Abstract: Hydrogen bond assisted ortho-selective C(sp2)-H amination of nitrosoarenes and subsequent α-C(sp3)-H functionalization of aliphatic amines is achieved under metal-free conditions. The annulation of nitrosoarenes and 2-hydroxy-C-nitroso compounds with N-heterocycles provides a facile excess to a… read more here.
Keywords: sp2 sp3; free sequential; ring fused; sequential sp2 ... See more keywords
Expanding the chemistry of ring-fused 1,4-diphosphinines by stable mono anion formation.
Sign Up to like & getrecommendations! Published in 2018 at "Chemical communications"
DOI: 10.1039/c8cc08158a
Abstract: A new sulfur-enriched tricyclic 1,4-diphosphinine (2) was synthesized and novel reactivity studies on the phosphorus heterocycle were performed: a weak anionic nucleophile (KHMDS) adds selectively thus forming a stable anionic 1,4-diphosphinine derivative (3b) which was… read more here.
Keywords: fused diphosphinines; ring fused; expanding chemistry; chemistry ... See more keywords
Ring-fused cyclobutanes via cycloisomerization of alkylidenecyclopropane acylsilanes†
Sign Up to like & getrecommendations! Published in 2020 at "Chemical Science"
DOI: 10.1039/d0sc02224a
Abstract: A novel Lewis acid-catalyzed cycloisomerization of alkylidenecyclopropane acylsilanes is disclosed. The readily available starting materials participate in tandem Prins addition/ring expansion/1,2-silyl shift to grant access to bicyclo[4.2.0]octanes and bicyclo[3.2.0]heptanes, which are common motifs in terpenoid… read more here.
Keywords: ring fused; alkylidenecyclopropane acylsilanes; cycloisomerization alkylidenecyclopropane; fused cyclobutanes ... See more keywords
High-performance five-ring-fused organic semiconductors for field-effect transistors.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical Society reviews"
DOI: 10.1039/d1cs01136g
Abstract: Organic molecular semiconductors have been paid great attention due to their advantages of low-temperature processability, low fabrication cost, good flexibility, and excellent electronic properties. As a typical example of five-ring-fused organic semiconductors, a single crystal… read more here.
Keywords: field effect; fused organic; ring fused; five ring ... See more keywords
Ring-fused hexahydro-1,2,4,5-tetrazines: synthesis, structure, and mechanistic studies on isolable rotational isomers.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc06170h
Abstract: We designed conformationally stable rotational isomers around the C(sp2)-C(sp3) axis at the C3-position of hexahydro-1,2,4,5-tetrazines. Isolation of each rotamer by silica gel column chromatography was successfully achieved at room temperature. The proposed isomerization mechanism of… read more here.
Keywords: ring fused; hexahydro tetrazines; rotational isomers; fused hexahydro ... See more keywords
Five-Membered-Ring-Fused Tacrines as Anti-Alzheimer’s Disease Agents
Sign Up to like & getrecommendations! Published in 2021 at "Synlett"
DOI: 10.1055/s-0040-1719823
Abstract: Our endeavors in the design, synthesis, and biological assessment of five-membered-ring-fused tacrines as potential therapeutic agents for Alzheimer’s disease are summarized. Particularly, we have identified racemic 4-(2-methoxyphenyl)-3-methyl-2,4,6,7,8,9-hexahydropyrazolo[4′,3′:5,6]pyrano[2,3-b]quinolin-5-amine, a pyranopyrazolotacrine, as having the best nontoxic profile… read more here.
Keywords: membered ring; ring fused; alzheimer disease; fused tacrines ... See more keywords
A Highly Substituted Ring-Fused 2-Pyridone Compound Targeting PrfA and the Efflux Regulator BrtA in Listeria monocytogenes
Sign Up to like & getrecommendations! Published in 2023 at "mBio"
DOI: 10.1128/mbio.00449-23
Abstract: Bacteria resistant to one or several antibiotics are a very large problem, threatening not only treatment of infections but also surgery and cancer treatments. Thus, new types of antibacterial drugs are desperately needed. ABSTRACT Listeria… read more here.
Keywords: ring fused; pyridone; cholic acid; listeria monocytogenes ... See more keywords
Hydrosilyl Group-directed Iridium-catalyzed peri-Selective C–H Borylation of Ring-fused (Hetero)Arenes
Sign Up to like & getrecommendations! Published in 2018 at "Chemistry Letters"
DOI: 10.1246/cl.180594
Abstract: The iridium-catalyzed direct C–H borylation of ring-fused (hetero)arenes afforded borylated products in a peri-selective manner, directed by a proximal hydrosilyl group. Further selective transformations of the boryl and silyl groups enabled the synthesis of various… read more here.
Keywords: ring fused; hetero arenes; iridium catalyzed; hetero ... See more keywords