27144-85-0Relevant academic research and scientific papers
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
, 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
Synthesis and Determination of Lipophilicity, Anticonvulsant Activity, and Preliminary Safety of 3-Substituted and 3-Unsubstituted N-[(4-Arylpiperazin-1-yl)alkyl]pyrrolidine-2,5-dione Derivatives
Rybka, Sabina,Obniska, Jolanta,?mudzki, Pawe?,Koczurkiewicz, Paulina,Wójcik-Pszczo?a, Katarzyna,P?kala, El?bieta,Bry?a, Adrian,Rapacz, Anna
, p. 1848 - 1856 (2017/11/20)
A new series of 1,3-substituted pyrrolidine-2,5-dione derivatives as potential anticonvulsant agents are described. Initial pharmacological screening of these compounds was performed by using acute models of seizures (MES and scPTZ tests) in mice after in
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
experimental part, 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
Accelerated Koenigs - Knorr Glucuronidation of a Deactivated Nitrophenol: Unveiling the Role of Polyamine Additive 1,1,4,7,10,10-Hexamethyltriethylenetetramine1 through Design of Experiments
Stazi, Federica,Palmisano, Giovanni,Turconi, Marco,Clini, Simona,Santagostino, Marco
, p. 1097 - 1103 (2007/10/03)
1,1,4,7,10,10-Hexamethyltriethylenetetramine (HMTTA) emerged from a limited parallel screening of selected polyamines as the most appropriate additive for an especially problematic Koenigs-Knorr glucuronidation. This initial finding rapidly evolved into a
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.
Quantitative structure-activity analyses of novel hydroxyphenylurea derivatives as antioxidants
Nakao, Kazuya,Shimizu, Ryo,Kubota, Hitoshi,Yasuhara, Mikiko,Hashimura, Yoshimasa,Suzuki, Toshikazu,Fujita, Toshio,Ohmizu, Hiroshi
, p. 849 - 868 (2007/10/03)
A series of substituted hydroxyphenylureas was synthesized, the chemical structure of which was designed based on structures of natural antioxidants, vitamin E (α-tocopherol) and uric acid. They exhibited high inhibitory activity against lipid peroxidation. In order to gain an insight into the mechanism of the inhibition reaction, we analyzed their structure-activity relationships quantitatively. Electronic and steric effects of substituents on the phenolic hydroxyl group were shown to be of importance in governing the inhibitory potency. An increase in the electron donating property of substituents toward the phenolic hydroxyl group enhanced the antioxidative activity by the stabilization of an electron-deficient radical-type transition state. The steric shielding by ortho-substituents stabilized the phenoxy radicals formed following the transition state. Derivatives having the carboxyl group were only weakly active presumably because of an intermolecular ion-dipole interaction of the phenolic hydroxyl group with the carboxylate anion which could retard the formation of the transition state. Copyright (C) 1998 Elsevier Science Ltd.
5-HT and DA receptor affinity of arylpiperazine derivatives with terminal benzamide fragment
Perrone,Berardi,Leopoldo,Tortorella,Lograno,Daniele,Govoni
, p. 567 - 572 (2007/10/02)
The synthesis of some arylpiperazines with a benzamide moiety on N-4 alkyl chain was accomplished and their dopaminergic and serotonergic affinity was assayed by in vitro receptor binding. The results of such investigation showed a moderate affinity on D-
