75000-29-2Relevant academic research and scientific papers
Benzyne-Induced Ring Opening Reactions of DABCO: Synthesis of 1,4-Disubstituted Piperazines and Piperidines
Seo, Jeongseob,Kim, Daegeun,Ko, Haye Min
supporting information, p. 2739 - 2743 (2020/05/25)
The 2-(4-phenylpiperazin-1-yl)ethan-1-amine scaffold is a structurally important motif that occurs frequently in medicinal and pharmaceutical chemistry. Despite the significance of this moiety, general strategies for its synthesis to date have required mu
Small-Molecule Inhibition of the UNC119–Cargo Interaction
Mejuch, Tom,Garivet, Guillaume,Hofer, Walter,Kaiser, Nadine,Fansa, Eyad K.,Ehrt, Christiane,Koch, Oliver,Baumann, Matthias,Ziegler, Slava,Wittinghofer, Alfred,Waldmann, Herbert
supporting information, p. 6181 - 6186 (2017/05/22)
N-Terminal myristoylation facilitates membrane binding and activity of proteins, in particular of Src family kinases, but the underlying mechanisms are only beginning to be understood. The chaperones UNC119A/B regulate the cellular distribution and signal
Chemical modifications on 4-arylpiperazine-ethyl carboxamide derivatives differentially modulate affinity for 5-HT1A, D4.2, and α2A receptors: Synthesis and in vitro radioligand binding studies
Graulich, Amaury,Lonard, Marc,Rsimont, Mlissa,Huang, Xi-Ping,Roth, Bryan L.,Ligeois, Jean-Franois
scheme or table, p. 56 - 67 (2010/05/18)
A series of substituted 4-aryl-piperazine-ethyl heteroarylcarboxamides were prepared and tested in in vitro radioligand binding studies. The presence of a quinoxaline has a favourable impact in terms of serotonin 5-HT1A versus dopamine D4.2 receptor selectivity. Compounds with a 3-CF3 group at the distal phenyl ring are the most effective in terms of affinity and selectivity for 5-HT1A versus D4.2 receptors. A 4-phenyl-1,2,3,6- tetrahydropyridine in place of the corresponding 4-phenyl-piperazine side chain is also favourable not only for the affinity for 5-HT1A and D4.2 receptors but also in some cases for α2A-adrenoceptors.
Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers
Lee, Jie Eun,Koh, Hun Yeong,Seo, Seon Hee,Baek, Yi Yeon,Rhim, Hyewhon,Cho, Yong Seo,Choo, Hyunah,Pae, Ae Nim
scheme or table, p. 4219 - 4222 (2010/09/04)
T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives subs
Synthesis and biological evaluation of novel T-type Ca2+ channel blockers
Jung, Hee Kyung,Doddareddy, Munikumar Reddy,Cha, Joo Hwan,Rhim, Hyewhon,Cho, Yong Seo,Koh, Hun Yeong,Jung, Bong Young,Pae, Ae Nim
, p. 3965 - 3970 (2007/10/03)
A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca 2+ channel. The compound 21 with trifluoromethyl substituents at C3-position of phenyl group (R1) and C2- position of phenyl group (R2) showed the highest inhibitory activity with IC50 value of 1.02μM, which is comparable to that of mibefradil.
Antipsychotic properties of new N-(4-substituted-1-piperazinylethyl)- and N-(4-substituted-1-piperidinylethyl)-phthalimides
Al-Rashood,Mustafa,Alhaider,Ginawi,Madani,El-Obeid
, p. 898 - 901 (2007/10/02)
A series of N-(4-phenyl- and 4-pyridyl-1-piperazinylethyl)- and N-(4-phenyl-1-piperidinylethyl)-phthalimides were synthesized and tested for antipsychotic activity. All compounds suppressed the spontaneous motor activity and the apomorphine-induced climbi
