97310-93-5Relevant academic research and scientific papers
DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
-
Page/Page column 109; 110, (2016/05/19)
The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
COMPOUNDS AND METHODS for the inhibition of HDAC
-
Paragraph 0449-0450, (2015/11/24)
Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
Catalytic Water Oxidation by a Molecular Ruthenium Complex: Unexpected Generation of a Single-Site Water Oxidation Catalyst
Rabten, Wangchuk,K?rk?s, Markus D.,?kermark, Torbj?rn,Chen, Hong,Liao, Rong-Zhen,Tinnis, Fredrik,Sun, Junliang,Siegbahn, Per E. M.,Andersson, Pher G.,?kermark, Bj?rn
, p. 4611 - 4620 (2015/05/27)
The increasing energy demand calls for the development of sustainable energy conversion processes. Here, the splitting of H2O to O2 and H2, or related fuels, constitutes an excellent example of solar-to-fuel conversion schemes. The critical component in such schemes has proven to be the catalyst responsible for mediating the four-electron oxidation of H2O to O2. Herein, we report on the unexpected formation of a single-site Ru complex from a ligand envisioned to accommodate two metal centers. Surprising N-N bond cleavage of the designed dinuclear ligand during metal complexation resulted in a single-site Ru complex carrying a carboxylate-amide motif. This ligand lowered the redox potential of the Ru complex sufficiently to permit H2O oxidation to be carried out by the mild one-electron oxidant [Ru(bpy)3]3+ (bpy = 2,2′-bipyridine). The work thus highlights that strongly electron-donating ligands are important elements in the design of novel, efficient H2O oxidation catalysts. (Chemical Equation Presented).
Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists
Sato, Nagaaki,Jitsuoka, Makoto,Ishikawa, Shiho,Nagai, Keita,Tsuge, Hiroyasu,Ando, Makoto,Okamoto, Osamu,Iwaasa, Hisashi,Gomori, Akira,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro
scheme or table, p. 1670 - 1674 (2009/11/30)
Novel imidazoline derivatives were discovered to be potent neuropeptide Y Y5 receptor antagonists. High-throughput screening of Merck sample collections against the human Y5 receptor resulted in the identification of 2,4,4-triphenylimidazoline (1), which had an IC50 of 54 nM. Subsequent optimization led to the identification of several potent derivatives.
4,6-DISUBSTITUTED PYRIMIDINES AND THEIR USE AS PROTEIN KINASE INHIBITORS
-
Page/Page column 58, (2008/06/13)
The invention relates to novel pyrimidine derivatives of Formula (I), which are efficacious inhibitors of protein kinases, in particular of one or more isoforms of the protein kinase B/Akt.
Copper-mediated oxidative C-terminal N-dealkylation of peptide-derived ligands. A possible model for enzymatic generation of desglycine peptide amides
Veera Reddy,Jin,Arora,Sfeir,Feke Malon ey,Urbach,Sayre
, p. 2332 - 2340 (2007/10/02)
A number of Cu(II) complexes of peptide derivatives that coordinate via N-deprotonation at the C-terminal amino acid residue have been characterized by tirimetry and the Cu(III)-Cu(II) electrochemical potentials. Reaction of these complexes with persulfate induces oxidative decarboxylation and hydrolysis of the resulting N-acylimines to carboxamide and either HCHO, CH3CHO, or acetone depending on the identity of the C-terminal residue (Gly, Ala, or Aib, respectively). For complexes with Cu(III)-Cu(II) potentials of +1.4 V vs NHE or lower, reaction with IrCl62- results in C-N dehydrogenation at the C-terminus, giving (after hydrolysis) carboxamide and either glyoxylic or pyruvic acid for C-terminal Gly or Ala. In the case of C-terminal Aib, Ir(IV) oxidation results in a very slow production of acetone. Complexes with E(p) above + 1.5 V do not react with IrCl62-6, and sarcosine-termianl complexes, as well as those containing phenolate ligation, are inert to both persulfate and Ir(IV). The optimal complex studied here for investigating the mechanism of C-N dehydrogenation was picolinyl-Aib-Ala (E(p) = +0.882 vs NHE), in which case the Ir(IV)-mediated cleavage to pyruvic acid and picolinyl-Aib-NH2 proceeds via a Cu(III) intermediate. The same transformation could be effected electrochemically. The C-terminal oxidative N-dealkylation reaction, induced by Cu(III), has not been previously observed and may be a relevant model for the copper enzyme peptidyl α-amidating monooxygenase, which is responsible for conversion of glycine-extended peptide prohormones to the biologically active peptide carboxamides.
Further Pyridine Derivatives Isolated from the Culture Medium of Pseudomonas putida - Genuine Metabolites or Artefacts?
Budzikiewicz, H.,Hildebrand, U.,Ockels, W.,Reiche, M.,Taraz, K.
, p. 516 - 520 (2007/10/02)
From the culture medium of Pseudomonas putida after treatment with CH2N2 besides the expected Pyridine-2,6-di(monothiocarboxylic acid)-di-S-methyl ester a series of pyridine derivatives could be isolated which could be shown to be artefacts formed from pyridine-2,6-di(monothiocarboxylic acid). - Keywords: Pyridine Derivatives, Bacterical Metabolites, Pseudomonas putida, Thiocarboxylic Acid Chemistry
