2887-55-0Relevant academic research and scientific papers
HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
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Page/Page column 102, (2015/01/16)
The present invention provides, in part, compounds of Formula (I) and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1 -mediated (or D1 -associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.
HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
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Page/Page column 88; 89, (2014/05/24)
The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β- arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.
Inhibitory effects of ethacrynic acid analogues lacking the α,β-unsaturated carbonyl unit and para-acylated phenols on human cancer cells
Bryant, Zack E.,Janser, Romy F.J.,Jabarkhail, Medina,Candelaria-Lyons, Melissa S.,Romero, Brittni B.,Slambrouck, Severine Van,Steelant, Wim F.A.,Janser, Ingo
scheme or table, p. 912 - 915 (2011/03/21)
A series of ethacrynic acid analogues, lacking the α,β- unsaturated carbonyl unit, was synthesized and subsequently evaluated for their ability to inhibit the migration of human breast cancer cells, Hs578Ts(i)8 as well as of human prostate cancer cells, C4-2B. These cell lines provide a good model system to study migration and invasion, since they represent metastatic cancer. Our studies show that ethacrynic acid analogues with methyl substituents at the aromatic ring demonstrate no inhibitory effect on the migration of both cancer cell lines, whereas a precursor in the synthesis of these ethacrynic acid analogues (II-1, a para-acylated m-cresol) is an excellent inhibitor of the migration of both cancer cell lines.
Comparisons of O-acylation and Friedel-Crafts acylation of phenols and acyl chlorides and Fries rearrangement of phenyl esters in trifluoromethanesulfonic acid: Effective synthesis of optically active homotyrosines
Murashige, Ryo,Hayashi, Yuka,Ohmori, Syo,Torii, Ayuko,Aizu, Yoko,Muto, Yasuyuki,Murai, Yuta,Oda, Yuji,Hashimoto, Makoto
experimental part, p. 641 - 649 (2011/03/19)
Reactions involving phenol derivatives and acyl chlorides have to be controlled for competitive O-acylations and C-acylations (Friedel-Crafts acylations and Fries rearrangements) in acidic condition. The extent for these reactions in trifluoromethanesulfonic acid (TfOH), which is used as catalyst and solvent, is examined. Although diluted TfOH was needed for effective O-acylation, concentrated TfOH was required for effective C-acylations in mild condition. These results have been applied to the novel synthesis of homotyrosine derivatives. Both Fries rearrangement of N-TFA-Asp(OBn)-OMe and Friedel-Crafts acylation of phenol with N-TFA-Asp(Cl)-OMe in TfOH afforded the homotyrosine skeleton, followed by reduction and deprotection afforded homotyrosines maintaining stereochemistry of Asp as an optically pure form.
Ethacrynic acid analogues lacking the α,β-unsaturated carbonyl unit-Potential anti-metastatic drugs
Janser, Romy F.J.,Meka, Ranjith K.,Bryant, Zack E.,Adogla, Enoch A.,Vogel, Elizabeth K.,Wharton, Jaimie L.,Tilley, Cynthia M.,Kaminski, Catherine N.,Ferrey, Seth L.,Van slambrouck, Severine,Steelant, Wim F.A.,Janser, Ingo
experimental part, p. 1848 - 1850 (2010/07/06)
A series of ethacrynic acid analogues, lacking the α,β-unsaturated carbonyl unit, was synthesized and subsequently evaluated for their ability to inhibit the migration of human breast cancer cells, MCF-7/AZ. Several of the analogues were already active in the low micromolar range, whereas ethacrynic acid itself shows no potential to inhibit the migration of these cancer cells. Preliminary studies show that the presence of one or more methoxy groups at the phenyl ring of ethacrynic acid is important in order for the ethacrynic acid analogues to demonstrate an inhibitory effect on the migration.
A comparative study: One pot synthesis of some prochiral ketones using conventional and microwave assisted methods
Salokhe,Mote,Suryavanshi,Salunkhe
experimental part, p. 1347 - 1351 (2010/07/05)
Polyphosphoric acid (PPA) has been used to synthesize a number of prochiral aryl ketones as well as α,β-unsaturated diaryl ketones by conventional and microwave assisted methods in moderate to good yield. The microwave assisted method is advantageous due to increased yield and high purity of products within incredible short period of time.
A new lead for nonpeptidic active-site-directed inhibitors of the severe acute respiratory syndrome coronavirus main protease discovered by a combination of screening and docking methods
Kaeppler, Ulrich,Stiefl, Nikolaus,Schiller, Markus,Vicik, Radim,Breuning, Alexander,Schmitz, Werner,Rupprecht, Daniel,Schmuck, Carsten,Baumann, Knut,Ziebuhr, John,Schirmeister, Tanja
, p. 6832 - 6842 (2007/10/03)
The coronavirus main protease, Mpro, is considered to be a major target for drugs suitable for combating coronavirus infections including severe acute respiratory syndrome (SARS). An HPLC-based screening of electrophilic compounds that was perf
Lewis Acids Catalysed Fries Rearrangement of Isopropylcresol Esters
Martin, Robert,Demerseman, Pierre
, p. 227 - 236 (2007/10/02)
In the course of the Fries rearrangement, aluminium chloride frequently induces migration or elimination of alkyl groups.The results obtained with titanium tetrachloride for the synthesis of vicinal o-hydroxyketones are compared with those obtained with aluminium chloride for some aliphatic and aromatic esters of isopropylcresols.In order to understand the migration and elimination processes occurring, the stabilities of the o-hydroxyketones are studied in the presence of aluminium chloride at different temperatures.Furthermore, all-vicinal o-hydroxyketones were prepared by the Fries rearrangement of 6-tert-butyl-p-thymol with titanium tetrachloride.
