827-24-7Relevant academic research and scientific papers
Relayed Regioselective Alkynylation/Olefination of Unsymmetrical Cyclic Diaryliodonium Species Catalyzed by Cu and Pd: Affording Fluorescent Cytotoxic Benzoxazoles
Zhu, Daqian,Liu, Panpan,Lu, Wenhua,Wang, Haiwen,Luo, Bingling,Hu, Yumin,Huang, Peng,Wen, Shijun
, p. 18915 - 18920 (2015)
Although cyclic diaryliodonium species have the potential to act as valuable synthons for cascade transformations, they still remain largely unexplored. The regioselectivity associated with unsymmetrical cyclic diaryliodonium species has previously been k
Benzotriazine compound with PAR4 antagonistic activity and application thereof
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Paragraph 0059; 0061; 0066, (2020/08/02)
The invention discloses a benzotriazine compound with PAR4 antagonistic activity and application thereof. The present invention relates to a compound of formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, ester, solvate or prodrug t
Effects of Thiolate Ligation in Monoiron Hydrogenase (Hmd): Stability of the {Fe(CO)2}2+ Core with NNS Ligands
Xie, Zhu-Lin,Pennington, Doran L.,Boucher, Dylan G.,Lo, James,Rose, Michael J.
, p. 10028 - 10039 (2018/08/28)
In this work, we report the effects of NNS-thiolate ligands and nuclearity (monomer, dimer) on the stability of iron complexes related to the active site of monoiron hydrogenase (Hmd). A thermally stable iron(II) dicarbonyl motif is the core feature of th
Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands
Szymańska, Ewa,Cha?upnik, Paulina,Szczepańska, Katarzyna,Cu?ado Moral, Ana Maria,Pickering, Darryl S.,Nielsen, Birgitte,Johansen, Tommy N.,Kie?-Kononowicz, Katarzyna
supporting information, p. 5568 - 5572 (2016/11/09)
A new series of carboxyaryl-substituted phenylalanines was designed, synthesized and pharmacologically characterized in vitro at native rat ionotropic glutamate receptors as well as at cloned homomeric kainate receptors GluK1–GluK3. Among them, six compounds bound to GluK1 receptor subtypes with reasonable affinity (Kivalues in the range of 4.9–7.5?μM). A structure–activity relationship (SAR) for the obtained series, focused mainly on the pharmacological effect of structural modifications in the 4- and 5-position of the phenylalanine ring, was established. To illustrate the results, molecular docking of the synthesized series to the X-ray structure of GluK1 ligand binding core was performed. The influence of individual substituents at the phenylalanine ring for both the affinity and selectivity at AMPA, GluK1 and GluK3 receptors was analyzed, giving directions for future studies.
Synthesis of 6,6′-bis(dimethylamino)- and 6,6′-dibromo- substituted 2,2′-diphosphanylbiphenyls and their palladium complexes
Petzold, Holm,Alrawashdeh, Albara I. S.,Heider, Silvio,Haufe, Linda,Rueffer, Tobias
, p. 4858 - 4866 (2013/09/24)
New 6,6′-dibromo- and 6,6′-bis(dimethylamino)-substituted 2,2′-diphosphanylbiphenyl ligands 11-14 were prepared starting from 2,2′-dibromo-4,4′-dimethyl-6,6′-dinitro-1,1′-biphenyl (4). Depending on the phosphane groups [diphenylphosphanyl (11, 13) or diis
The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea group
Procopiou, Panayiotis A.,Barrett, Victoria J.,Ford, Alison J.,Looker, Brian E.,Lunniss, Gillian E.,Needham, Deborah,Smith, Claire E.,Somers, Graham
experimental part, p. 6026 - 6032 (2011/11/07)
A series of novel, potent and selective human β2 adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of (R)-salmeterol is presented. Urea 9j had long duration of action in vitro on guinea pig trachea, and also in vivo similar to that of salmeterol. It had lower oral absorption and bioavailability than salmeterol in both rat and dog. It had a turnover ratio similar to salmeterol, with no evidence for formation of any aniline metabolites in human liver microsomes and hepatocytes. However no crystalline salts suitable for inhaled delivery were identified.
Synthesis of 4,4′-bisaryl-2,2′-bisbenzimidazoles as building blocks for supramolecular structures
Yasui, Yoshizumi,Frantz, Derik K.,Siegel, Jay S.
, p. 4989 - 4992 (2007/10/03)
(Chemical Equation Presented) A series of 4,4′-bisaryl-2,2′- bisbenzimidazoles has been synthesized from the corresponding 4,4′-dibromo-2,2′-bisbenzimidazoles by Negishi coupling reactions. This procedure affords highly substituted bisbenzimidazoles.
PHENETHANOLAMINE DERIVATIVES FOR TREATMENT OF RESPIRATORY DISEASES
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Page/Page column 78, (2010/02/07)
The present invention relates to novel compounds of formula (I),to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.
Benzo[1,2-c]1,2,5-oxadiazole N-Oxide Derivatives as Potential Antitrypanosomal Drugs. Structure-Activity Relationships. Part II
Aguirre, Gabriela,Cerecetto, Hugo,Maio, Rossanna Di,Gonzalez, Mercedes,Porcal, Williams,Seoane, Gustavo,Ortega, Miguel A.,Aldana, Ignacio,Monge, Antonio,Denicola, Ana
, p. 15 - 21 (2007/10/03)
The preparation of new derivatives of benzo[1,2-c]1,2,5-oxadiazole N-oxide is described. These derivatives were chosen in order to investigate and confirm previous structural features found necessary to display an adequate antitrypanosomal activity. The c
Oxidative Bromination of Aromatic Amides using Sodium Perborate as Oxidant
Hanson, James R.,Harpel, Simone,Medina, Inmaculada C. Rodriguez,Rose, Dorian
, p. 432 - 433 (2007/10/03)
Sodium perborate in glacial acetic acid-acetic anhydride with potassium bromide and sodium tungstate as a catalyst, provides a novel system for the bromination of aromatic amides.
