- Paramagnetic ruthenium(III) complexes bearing O,O chelating ligands: Synthesis, spectra, molecular structure and electron transfer properties
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Paramagnetic Ru(III) complexes of the type [RuX2(EPh 3)2(L)] (where X = Cl or Br; E = P or As; L = monobasic bidentate benzophenone ligand) have been synthesized from the reaction of ruthenium(III) precursors, viz. [RuX3(EPh3)3] (where X = Cl, E = P; X = Cl or Br, E = As) or [RuBr3(PPh 3)2(CH3OH)] and substituted hydroxy benzophenones in a 1:1 molar ratio in benzene under reflux for 6 h. The hydroxy benzophenone ligands behave as monoanionic bidentate O,O donors and coordinate to ruthenium through the phenolate oxygen and ketonic oxygen atoms, generating a six-membered chelate ring. The compositions of the complexes have been established by analytical and spectral (FT-IR, UV-Vis, EPR) and X-ray crystallography methods. The single crystal structure of the complex [RuCl 2(PPh3)2(L1)] (1) has been determined by X-ray crystallography and indicates the presence of a distorted octahedral geometry in these complexes. The magnetic moment values of the complexes are in the range 1.75-1.89 μB, which reveals the presence of one unpaired electron in the metal ion. EPR spectra of liquid samples at liquid nitrogen temperature (LNT) show a rhombic distortion (g x ≠ gy ≠ gz) around the ruthenium ion. The complexes are redox active and display quasi-reversible oxidation and quasi-reversible reduction waves versus Ag/AgCl.
- Raja, Nandhagopal,Ramesh, Rengan,Liu, Yu
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p. 196 - 201
(2012/03/11)
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- Discovery of a potent and orally available acyl-CoA: Cholesterol acyltransferase inhibitor as an anti-atherosclerotic agent: (4-Phenylcoumarin) acetanilide derivatives
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Acyl-CoA: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes cholesterol esterification. ACAT inhibitors are expected to be potent therapeutic agents for the treatment of atherosclerosis. A series of potent ACAT inhibitors based on an (4-phenylcoumarin)acetanilide scaffold was identified. Evaluation of the structure-activity relationships of a substituent on this scaffold, with an emphasis on improving the pharmacokinetic profile led to the discovery of 2-[7-chloro-4-(3-chlorophenyl)-6-methyl-2-oxo-2H-chromen-3- yl]-N-[4-chloro-2-(trifluoromethyl)phenyl]acetamide (23), which exhibited potent ACAT inhibitory activity (IC50=12 nM) and good pharmacokinetic profile in mice. Compound 23 also showed regressive effects on atherosclerotic plaques in apolipoprotein (apo)E knock out (KO) mice at a dose of 0.3 mg/kg per os ( p.o.).
- Ogino, Masaki,Fukui, Seiji,Nakada, Yoshihisa,Tokunoh, Ryosuke,Itokawa, Shigekazu,Kakoi, Yuichi,Nishimura, Satoshi,Sanada, Tsukasa,Fuse, Hiromitsu,Kubo, Kazuki,Wada, Takeo,Marui, Shogo
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p. 1268 - 1273
(2011/11/06)
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- Method of treating inflammation
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A method of treating inflammation and inhibiting prostaglandin synthesis employing 2-hydroxybenzophenone and substituted 2-hydroxybenzophenones.
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