84347-67-1Relevant academic research and scientific papers
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains
Jecs, Edgars,Miller, Eric J.,Wilson, Robert J.,Nguyen, Huy H.,Tahirovic, Yesim A.,Katzman, Brook M.,Truax, Valarie M.,Kim, Michelle B.,Kuo, Katie M.,Wang, Tao,Sum, Chi S.,Cvijic, Mary E.,Schroeder, Gretchen M.,Wilson, Lawrence J.,Liotta, Dennis C.
supporting information, p. 89 - 93 (2018/02/19)
A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXCR4 inhi
NOVEL DOPAMINE D3 RECEPTOR LIGANDS, THE PREPARATION AND USE THEREOF
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Page/Page column 15, (2011/09/12)
The invention discloses novel piperazine derivatives represented by formula I having activity for modulating dopamine D3 receptor, their stereoisomers, pharmaceutical salts, solvates, and the pharmaceutical compositions containing such compounds, their preparation and the use of such compounds for preventing or treating the diseases correlated with central nervous system disorder, such as Parkinson's disease, schizophrenia, drug addiction and relapse and the like, as well as the use of such compounds for kidney protection and immune modulation, or as implemental medicine for researching the function of D3R and the diseases correlated with disorder of D3R function.
NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME
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Page/Page column 9, (2012/01/13)
The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson''s disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
Application of a chiral scaffolding ligand in catalytic enantioselective hydroformylation
Worthy, Amanda D.,Joe, Candice L.,Lightburn, Thomas E.,Tan, Kian L.
supporting information; experimental part, p. 14757 - 14759 (2010/12/19)
The synthesis of β-amino-aldehydes has been achieved through enantioselective hydroformylation of PMP-protected allylic amines. The reaction is accomplished by using a scalemic scaffolding ligand that covalently and reversibly binds to the substrate. These ligands behave like chiral auxiliaries because they are covalently attached to the substrate during hydroformylation; however, similar to traditional asymmetric ligands, they can be used in catalytic quantities. The directed hydroformylation of disubstituted olefins occurs under mild conditions (35 °C and 50 psi CO/H2), and Z-olefins afford excellent enantioselectivities (up to 93% ee).
The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands
Bojarski, Andrzej J.,Duszyńska, Beata,Ko?aczkowski, Marcin,Kowalski, Piotr,Kowalska, Teresa
, p. 5863 - 5866 (2007/10/03)
New cis-, trans-2-butene and 1,2-bismethylbenzene analogues of MM77 and NAN-190 (1-{4-[4-(2-methoxyphenyl)-piperazin-1-yl]-butyl}-pyrrolidine-2,5-dione and isoindole-1,3-dione, respectively) were synthesized. The differences in their in vitro affinity for serotonin 5-HT7 and 5-HT1A receptors were explained using a conformational analysis. A bioactive conformation of those compounds for the 5-HT7 receptor, different from that established for 5-HT1A, was proposed.
N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl}arylcarboxamides as novel dopamine D3 receptor antagonists
Newman, Amy Hauck,Cao, Jianjing,Bennett, Christina J.,Robarge, Michael J.,Freeman, Rebekah A.,Luedtke, Robert R.
, p. 2179 - 2183 (2007/10/03)
The dopamine D3 receptor subtype has been targeted as a potential neurochemical modulator of the behavioral actions of psychomotor stimulants, such as cocaine. Previous synthetic studies provided structural requirements for high affinity bindin
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives
Norman, Mark H.,Minick, Douglas J.,Rigdon, Greg C.
, p. 149 - 157 (2007/10/03)
A series of phthalimide and isoindolinone derivatives bridged to 4-(1,2- benzisothiazol-3-yl)-1-piperazinyl was prepared. The compounds were evaluated in vitro at dopamine D2 and serotonin 5-HT(1a) and 5-HT2 receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. The effects of bridge length and conformation on the biological activity of these potential antipsychotic agents are discussed. A four-carbon spacer provided optimal activity within the two homologous series. Conformational investigations of the lead compound, isoindolinone 2, were conducted in an attempt to account for the superior activity observed for the butyl derivatives. On the basis of NMR and molecular modeling studies, two types of folded structures were proposed and several conformationally restrained analogues were synthesized. In general, restrictions incorporated within the linking bridge were detrimental to activity.
