59803-36-0Relevant academic research and scientific papers
4-alkyloxyimino derivatives of uridine-5′-triphosphate: Distal modification of potent agonists as a strategy for molecular probes of P2Y 2, P2Y4, and P2Y6 receptors
Jayasekara, P. Suresh,Barrett, Matthew O.,Ball, Christopher B.,Brown, Kyle A.,Hammes, Eva,Balasubramanian, Ramachandran,Harden, T. Kendall,Jacobson, Kenneth A.
, p. 3874 - 3883 (2014/05/20)
Extended N4-(3-arylpropyl)oxy derivatives of uridine-5′-triphosphate were synthesized and potently stimulated phospholipase C stimulation in astrocytoma cells expressing G protein-coupled human (h) P2Y receptors (P2YRs) activated by UTP (P2Y2/4R) or UDP (P2Y6R). The potent P2Y4R-selective N4-(3- phenylpropyl)oxy agonist was phenyl ring-substituted or replaced with terminal heterocyclic or naphthyl rings with retention of P2YR potency. This broad tolerance for steric bulk in a distal region was not observed for dinucleoside tetraphosphate agonists with both nucleobases substituted. The potent N 4-(3-(4-methoxyphenyl)-propyl)oxy analogue 19 (EC50: P2Y2R, 47 nM; P2Y4R, 23 nM) was functionalized for chain extension using click tethering of fluorophores as prosthetic groups. The BODIPY 630/650 conjugate 28 (MRS4162) exhibited EC50 values of 70, 66, and 23 nM at the hP2Y2/4/6Rs, respectively, and specifically labeled cells expressing the P2Y6R. Thus, an extended N4-(3- arylpropyl)oxy group accessed a structurally permissive region on three G q-coupled P2YRs, and potency and selectivity were modulated by distal structural changes. This freedom of substitution was utilized to design of a pan-agonist fluorescent probe of a subset of uracil nucleotide-activated hP2YRs.
NOVEL MALONIC ACID SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Page/Page column 51, (2010/04/25)
The present invention provides a novel compound having an agonist action at AT2 receptor and expected as a pharmaceutical product, and also provides a method of treating or preventing various diseases. The novel sulfonyl malonamide derivative,
Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the b2 adrenergic receptor
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Page/Page column 30, (2009/09/26)
The present invention provides a compound of formula (I): wherein: R1 is a group selected from -CH2OH,-NHCOH and R2 is a hydrogen atom; or R1 together with R2 form the group -NHC(O)CH=CH-, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2, R3a and R3b are independently selected from the group consisting of hydrogen atoms and C1-4 alkyl groups n is an integer selected from 0 to 6, R4 is selected from the group consisting of an optionally substituted monocyclic or polycyclic C3-10 cycloalkyl group, an optionally substituted monocyclic C5-10 aryl group and, a methyl group which is substituted with one or more substituents selected from C5-10 aryl and C5-10 aryloxy groups, wherein the monocyclic or polycyclic C3-10 cycloalkyl and the monocyclic C5-10 aryl groups independently are optionally substituted with one or more substituents selected from halogen atoms, C1-4 alkyl, C1-4 alkoxy, C5-10 aryl and C5-10 aryloxy groups, or a pharmaceutically-acceptable salt or solvate or stereoisomer thereof.
Modified pyrimidine glucocorticoid receptor modulators
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Page/Page column 16, (2008/06/13)
The present invention provides a novel class of modified pyrimidine compounds and compositions and methods of using the compounds as glucocorticoid receptor modulators.
Synthesis of Substituted Tetrahydronaphthalenes by Mn(III), Ce(IV), and Fe(III) Oxidation of Substituted Diethyl α-Benzylmalonates in the Presence of Olefins
Citterio, Attilio,Sebastiano, Roberto,Marion, Antonio,Santi, Roberto
, p. 5328 - 5335 (2007/10/02)
The oxidation of substituted diethyl α-benzylmalonates (1a-m) by manganese(III) acetate in acetic acid, cerium(IV) ammonium nitrate in methanol, or iron(III) perchlorate in acetonitrile in the presence of substituted olefins 2a-u was investigated.The results are consistent with a common mechanism.It involves selective generation of malonyl radicals from high-valent metal malonyl complexes, their addition to the olefin, and competition of the adduct radical between intramolecular cyclization to produce highly functionalized tetrahydronaphthalenes (3) and oxidation bymetal salt to give mainly γ-lactones (5).Several electron-withdrawing and releasing substituents on the aromatic ring and on the olefin can be successfully used in the synthesis of 3 without olefin telomerization.The influence of metal and olefin or aromatic substituents on the homolytic addition and intramolecular aromatic substitution is discussed.
