17135-46-5Relevant academic research and scientific papers
The search of novel inhibitors of HIV-1 Integrase among 5-(4-Halogenophenyl)-5-oxopentyl derivatives of nucleic bases
Komissarov,Knyazhanskaya,Atrokhova,Gottikh,Kritzyn
, p. 532 - 540 (2014)
New nucleic base derivatives were obtained by alkylation of uracil, thymine, cytosine, adenine, 6-chloropurine, and 2-Amino-6-chloropurine with 5-chloro-1-(4-halogenophenyl)-1-pentanones, and their physical and chemical properties were studied. The influe
In-situ-generation of alkylsilyl peroxides from alkyl hydroperoxides and their subsequent copper-catalyzed functionalization with organosilicon compounds
Xu, Weiping,Zhong, Wenfeng,Yang, Qin,Kato, Terumasa,Liu, Yan,Maruoka, Keiji
supporting information, (2021/06/16)
Alkylsilyl peroxides were generated in situ from the corresponding alkyl hydroperoxides using organosilicon compounds of the type Me3SiX (X = CN, N3, and halogens) and an amine base. Subsequent in situ copper-catalyzed homolytic cleavage of the alkylsilyl peroxides afforded alkyl radicals, which were then trapped with X (X = CN, N3, and halogens) to furnish products with new carbon-carbon, carbon-nitrogen, or carbon-halogen bonds in good to high yields.
Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor
Fyfe, Tim J.,Kellam, Barrie,Sykes, David A.,Capuano, Ben,Scammells, Peter J.,Lane, J. Robert,Charlton, Steven J.,Mistry, Shailesh N.
, p. 9488 - 9520 (2019/11/11)
Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side effects (EPSs) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with contrasting kinetic profiles. Haloperidol displays fast association/slow dissociation at the D2R, whereas clozapine exhibits relatively slow association/fast dissociation. Recently, we have provided evidence that slow dissociation from the D2R predicts hyperprolactinemia, whereas fast association predicts EPS. Unfortunately, clozapine can cause severe side effects independent of its D2R action. Our results suggest an optimal kinetic profile for D2R antagonist APDs that avoids EPS. To begin exploring this hypothesis, we conducted a structure-kinetic relationship study of haloperidol and revealed that subtle structural modifications dramatically change binding kinetic rate constants, affording compounds with a clozapine-like kinetic profile. Thus, optimization of these kinetic parameters may allow development of novel APDs based on the haloperidol scaffold with improved side-effect profiles.
HDAC6 SELECTIVE INHIBITORS, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
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Paragraph 0107, (2019/11/28)
Compounds serving as histone deacetylase 6 (HDAC6) selective inhibitors, and applications thereof in the preparation of drugs for treating HDAC6-related diseases. Specifically disclosed are a compound as represented by formula (I) and a pharmaceutically acceptable salt thereof.
Regioselective Synthesis of Carbonyl-Containing Alkyl Chlorides via Silver-Catalyzed Ring-Opening Chlorination of Cycloalkanols
Huang, Feng-Qing,Xie, Jian,Sun, Jian-Guo,Wang, Yue-Wei,Dong, Xin,Qi, Lian-Wen,Zhang, Bo
supporting information, p. 684 - 687 (2016/03/01)
A novel and regioselective approach to carbonyl-containing alkyl chlorides via silver-catalyzed ring-opening chlorination of cycloalkanols is reported. Concurrent C(sp3)-C(sp3) bond cleavage and C(sp3)-Cl bond formation efficiently occur with good yields under mild conditions, and the chlorinated products are readily transformed into other useful synthetic intermediates and drugs. The reaction features complete regioselectivity, high efficiency, and excellent practicality. (Chemical Equation Presented).
Novel compound capable of activating Nrf2, and pharmaceutical compositions comprising the same
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Paragraph 0549; 0554-0556, (2016/10/08)
The present invention provides a novel compound which can activate Nrf2 that is a transcription factor for expression of the quinone reductase gene. Therefore the compound is effective for inhibiting apoptosis and preventing and treating brain nerve disea
