2122-63-6Relevant academic research and scientific papers
Solid-phase synthesis of heterocycles via palladium-catalyzed annulation
Wang, Yao,Huang, Tai-Nang
, p. 9605 - 9608 (1998)
Solid-phase linked o-iodoanilines (4) and o-iodophenol (9) reacted with 1,3- and 1,4-dienes in the presence of palladium acetate to generate highly substituted indolines, tetrahydroquinolines, hydrobenzofurans and hydrobenzopyrans, which provided an effic
KI-VO(acac)2-H2O2-acoh, A new iodinating system for selective iodination at C-5 position of activated pyrimidinediones: A combined experimental and density functional study
Saikia, Lakhinath,Talukdar, Dhrubajyoti,Deka, Ramesh C.,Thakur, Ashim J.
, p. 1031 - 1038 (2013)
KI-VO(acac)2-H2O2 in aqueous ethanolic medium with acetic acid as additive has been found to iodinate pyrimidinediones and aromatic amines. The methodology is mild, efficient, and environmentally benign. Density functional theory-based reactivity parameters support the experimentally observed reactivity of pyrimidinedione derivatives.
Spin system assignment of homo-o-phenylene ethynylene oligomers
Slutsky, Morris M.,Jones, Ticora V.,Tew, Gregory N.
, p. 342 - 347 (2007)
We previously reported the synthesis and solution characterization of short o-phenylene ethynylene (oPE) foldamers. Proton correlation techniques are not adequate for NMR assignment in these compounds as the ethynylene linkers interrupt proton connectivit
Novel multitarget-directed ligands targeting acetylcholinesterase and σ1 receptors as lead compounds for treatment of Alzheimer's disease: Synthesis, evaluation, and structural characterization of their complexes with acetylcholinesterase
Lalut, Julien,Santoni, Gianluca,Karila, Delphine,Lecoutey, Cédric,Davis, Audrey,Nachon, Florian,Silman, Israel,Sussman, Joel,Weik, Martin,Maurice, Tangui,Dallemagne, Patrick,Rochais, Christophe
, p. 234 - 248 (2018/11/24)
Pleiotropic intervention may be a requirement for effective limitation of the progression of multifactorial diseases such as Alzheimer's Disease. One approach to such intervention is to design a single chemical entity capable of acting on two or more targets of interest, which are accordingly known as Multi-Target Directed Ligands (MTDLs). We recently described donecopride, the first MTDL able to simultaneously inhibit acetylcholinesterase and act as an agonist of the 5-HT4 receptor, which displays promising activities in vivo. Pharmacomodulation of donecopride allowed us to develop a novel series of indole derivatives possessing interesting in vitro activities toward AChE and the σ1 receptor. The crystal structures of complexes of the most promising compounds with Torpedo californica AChE were solved in order to further understand their mode of inhibition.
Regioselective iodination of aryl amines using 1,4-dibenzyl-1,4-diazoniabicyclo [2.2.2] octane dichloroiodate in solution and under solvent-free conditions
Alikarami, Mohammad,Nazarzadeh, Somayeh,Soleiman-Beigi, Mohammad
, p. 157 - 162 (2015/01/30)
1,4-Dibenzyl-1,4-diazoniabicyclo[2.2.2]octane dichloroiodate is an efficient and regioselective reagent for iodination of aryl amines. A wide variety of aryl amines in reaction with this reagent afforded regioselectively iodinated products. The iodination reaction can be carried out in solution or under solvent-free condition at room temperature.
Heteroaryl carboxamides
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Page/Page column 11, (2015/11/16)
The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentrati
Ground-state elevation approach to suppress side reactions in gold-sensing systems based on alkyne activation
Seo, Hyewon,Jun, Mi Eun,Ranganathan, Koteeswari,Lee, Kyung-Ha,Kim, Kyong-Tai,Lim, Woocherl,Rhee, Young Min,Ahn, Kyo Han
supporting information, p. 1374 - 1377 (2014/04/03)
A novel approach to suppress the side reactions observed in the reaction-based gold-sensing systems based on the alkyne activation is disclosed. By elevating steric strain around the reaction site, the gold ion promoted ring-opening process in rhodamine-l
Synthesis of highly efficient pH-sensitive DNA cleaving aminomethyl N-substituted cyclic enediyne and its L-lysine conjugate
Hatial, Ishita,Addy, Partha S.,Ghosh, Ananta K.,Basak, Amit
supporting information, p. 854 - 857 (2013/03/13)
Two 10-membered benzo-fused N-substituted cyclic enediynes, one an amino methyl and the other, a C-lysine conjugated derivative 2 and 3, respectively were synthesized (as a 1.2:1 mixture of regioisomers) and their DNA-cleavage efficiency studied. Both the compounds showed much better DNA-cleavage profile than that of the parent unsubstituted enediyne 1. The lysine conjugate 3 showed an efficient pH dependent cleavage to the extent of ~50% of linear DNA formation under ambient conditions.
BICYCLIC DERIVATIVES USEFUL AS INHIBITORS OF DPP-1
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Page/Page column 30, (2011/07/06)
The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
Synthesis and evaluation of a series of C5′-substituted duocarmycin SA analogs
Robertson, William M.,Kastrinsky, David B.,Hwang, Inkyu,Boger, Dale L.
supporting information; experimental part, p. 2722 - 2725 (2011/07/06)
The synthesis and evaluation of a key series of analogs of duocarmycin SA, bearing a single substituent at the C5′ position of the DNA binding subunit, are described.
