59223-73-3Relevant articles and documents
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.
FUNGICIDAL BENZYLPYRIMIDINE DERIVATIVES
-
Page/Page column 18, (2010/11/25)
Novel benzylpyrimidine derivatives of the formula (I) wherein, R represents C2-6 alkyl, X represents halogen, Y represents halogen, and n is an integer of 0 to 2, when n is 2 the two Y radicals may be the same or different from each other, and
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.
