214971-09-2Relevant articles and documents
Visible Light Induced Cyclization to Spirobi[indene] Skeletons from Functionalized Alkylidienecyclopropanes
Li, Quanzhe,Liu, Jiaxin,Shi, Min,Wei, Yin
supporting information, (2020/03/26)
In this paper, we revealed a metal-free and visible light photoinduced method for the rapid construction of spirobi[indene] skeletons, providing a simple and efficient way for easy access to spirobi[indene] scaffolds under mild conditions along with a broad substrate scope and good functional group tolerance.
Synthesis of Diiodinated All-Carbon 3,3′-Diphenyl-1,1′-spirobiindene Derivatives via Cascade Enyne Cyclization and Electrophilic Aromatic Substitution
Li, Quanzhe,Yu, Liuzhu,Wei, Yin,Shi, Min
supporting information, p. 9282 - 9296 (2019/08/12)
A synthetic method for the construction of diiodinated all-carbon spirobiindene derivatives has been developed from the reaction of propargyl alcohol-tethered alkylidenecyclopropanes with iodine. The reaction proceeded through an iodination-initiated cascade intramolecular enyne cyclization and electrophilic aromatic substitution reaction process in 1,2-dichloroethane upon heating, giving desired spirocyclic products in moderate to excellent yields. Further transformation of the obtained products has also been presented.
Palladium-Catalyzed Cascade Reductive and Carbonylative Cyclization of Ortho-Iodo-Tethered Methylenecyclopropanes (MCPs) Using N-Formylsaccharin as CO Source
Fan, Xing,Shi, Min,Wei, Yin
supporting information, p. 5677 - 5683 (2019/11/16)
A palladium-catalyzed reductive and carbonylative cyclization of ortho-iodo-tethered methylenecyclopropanes (MCPs) using N-formylsaccharin as CO source has been developed, affording the desired indanone derivatives in moderate to good yields with high regio- and stereoselectivity and good functional group compatibility.
Lewis or Br?nsted acid-catalysed reaction of propargylic alcohol-tethered alkylidenecyclopropanes with indoles and pyrroles for the preparation of polycyclic compounds tethered with indole or pyrrole motif
Wei, Hao-Zhao,Yu, Liu-Zhu,Shi, Min
supporting information, p. 135 - 139 (2019/12/26)
We developed a facile synthetic method to access cyclopenta[b]naphthalene derivatives via the Lewis or Br?nsted acid catalysed cascade nucleophilic addition, electronic cyclization, ring-opening rearrangement of propargylic alcohol-tethered alkylidenecyclopropanes with indole and pyrrole derivatives. The reaction exhibited a broad substrate scope and good functional group tolerance under metal-free conditions, affording the desired products in moderate to good yields.
Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists
Acker, Timothy M.,Khatri, Alpa,Vance, Katie M.,Slabber, Cathryn,Bacsa, John,Snyder, James P.,Traynelis, Stephen F.,Liotta, Dennis C.
supporting information, p. 6434 - 6456 (2013/09/23)
Here we describe the synthesis and structure-activity relationship for a class of pyrazoline-containing dihydroquinolone negative allosteric modulators of the NMDA receptor that show strong subunit selectivity for GluN2C- and GluN2D-containing receptors over GluN2A- and GluN2B-containing receptors. Several members of this class inhibit NMDA receptor responses in the nanomolar range and are more than 50-fold selective over GluN1/GluN2A and GluN1/GluN2B NMDA receptors, as well as AMPA, kainate, GABA, glycine, nicotinic, serotonin, and purinergic receptors. Analysis of the purified enantiomers of one of the more potent and selective compounds shows that the S-enantiomer is both more potent and more selective than the R-enantiomer. The S-enantiomer had an IC 50 of 0.17-0.22 μM at GluN2D- and GluN2C-containing receptors, respectively, and showed over 70-fold selectivity over other NMDA receptor subunits. The subunit selectivity of this class of compounds should be useful in defining the role of GluN2C- and GluN2D-containing receptors in specific brain circuits in both physiological and pathophysiological conditions.
COMPOUNDS WHICH INCREASE APOLIPOPROTEIN A-1 PRODUCTION AND USES THEREOF IN MEDICINE
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Page/Page column 32, (2010/10/20)
The present invention relates to compounds of formula (I), pharmaceutically acceptable salts thereof, hydrates thereof, solvates thereof, prodrugs thereof and combinations thereof: wherein X represents CH or N; Y represents CH or N; R1 represents H or C1-2alkyl; R2 represents H or C1-4alkyl; R3 represents C1-6alkyl, carbocyclyl, carbocyclylC1-4alkyl, heterocyclyl or heterocyclylC1-4alkyl, wherein any of the carbocyclyl or heterocyclyl groups are optionally substituted by one or two groups selected from: halogen, C1-6alkyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, nitro, cyano, -COH, -COOH, C1-6alkoxycarbonyl, C1-6alkylcarbonyl, -C(OH)R5R6 (wherein R5 and R6 independently represent H or C1-6alkyl), -(CH2)nNR3aR3b and -O(CH2)pNR3aR3b (wherein n represents 1, 2 or 3, p represents 2 or 3 and R3a and R3b independently represent H, C1-6alkyl or carbocyclylC1-4alkyl, or R3a and R3b together with the interconnecting atoms form a 5 or 6-membered ring which ring optionally contains one or two heteroatoms independently selected from the group consisting of O, S and N); R4 represents H, hydroxy, halo, C 1-6 alkyl, haloC1-6alkyl, hydroxyC1-6alkyl, C2-6alkenyl, C1-6alkoxy, haloC1-6alkoxy, carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl group is optionally substituted by one or two groups selected from: halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, nitro and cyano; and provided that the compound is not: 7-chloro-5-phenyl-[1,2,4]triazolo[4,3-a]quinolin-4-amine; 7-chloro-1-methyl-5-phenyl[1,2,4]triazolo[4,3-a]quinolin-4-amine; or 7-chloro-5-(2-chlorophenyl)-1-methyl-{1,2,4]triazolo[4,3-a]quinolin-4-amine. Also disclosed are pharmaceutical compositions containing the compounds and to their use in medicine. The compound exhibit increased apo-A1 production and are useful in the treatment for example a disease or condition caused by raised levels of LDL-cholesterol or by inflammation.
1,4-Benzodiazepines as inhibitors of respiratory syncytial virus
Carter, Malcolm C.,Alber, Dagmar G.,Baxter, Robert C.,Bithell, Sian K.,Budworth, Jo,Chubb, Ann,Cockerill, G. Stuart,Dowdell, Verity C. L.,Henderson, Elisa A.,Keegan, Sally J.,Kelsey, Richard D.,Lockyer, Michael J.,Stables, Jeremy N.,Wilson, Lara J.,Powell, Kenneth L.
, p. 2311 - 2319 (2007/10/03)
Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract infections worldwide and is increasingly being recognized as a serious threat to patient groups with poorly functioning immune systems. Our approach to finding a novel inhibitor of this virus was to screen a 20 000-member diverse library in a whole cell XTT assay. Parallel assays were carried out in the absence of virus in order to quantify any associated cell toxicity. This identified 100 compounds with IC50's less than 50 μM. A-33903 (18), a 1,4-benzodiazepine analogue, was chosen as the starting point for lead optimization. This molecule was moderately active and demonstrated good pharmacokinetic properties. The most potent compounds identified from this work were A-58568 (47), A-58569 (44), and A-62066 (46), where modifications to the aromatic substitution enhanced potency, and A-58175 (42), where the amide linker was modified.
