3935-51-1Relevant academic research and scientific papers
Synthesis of 4-(3-oxo-3-phenylpropyl)morpholin-4-ium chloride analogues and their inhibitory activities of nitric oxide production in lipopolysaccharide-induced BV2 cells
Yoon, Sung-Hwa,Lee, Eunhwa,Cho, Duk-Yeon,Ko, Hyun Myung,Baek, Ha Yeon,Choi, Dong-Kug,Kim, Eunha,Park, Ju-Young
supporting information, (2021/02/02)
Based on our previous report that 3-morpholino-1-phenylpropan-1-one 2, one of the fluoxetine's simplified morpholino analogue, inhibited nitric oxide (NO) production, in this paper, various substituted benzene analogues with morpholine hydrochloride of 2 were synthesized and their inhibitory effects on NO production in lipopolysaccharide (LPS)-induced BV2 cells were tested. Among the synthesized compounds, 2-trifluoromethyl analogue 16n (IC50 = 8.6 μM) showed a significantly higher inhibitory activity than that of the parent compound 2a (IC50 > 50 μM) and suppressed NO production dose-dependently without cytotoxicity. Compound 16n also inhibited iNOS expression in LPS-induced BV2 cells at 2, 10 and 20 μM concentrations. These results suggest that compound 16n inhibited NO production by suppressing the expression of iNOS and can be used as a lead structure for developing new inhibitor of NO production.
Photophysical properties and OLED performance of light-emitting platinum(ii) complexes
Kourkoulos, Dimitrios,Karakus, Cüneyt,Hertel, Dirk,Alle, Ronald,Schmeding, Sebastian,Hummel, Johanna,Risch, Nikolaus,Holder, Elisabeth,Meerholz, Klaus
supporting information, p. 13612 - 13621 (2013/09/23)
The synthesis, photophysical properties and application as emitters in solution-processed multi-layer organic light-emitting diodes (OLEDs) of a series of blue-green to red light-emitting phosphorescent platinum(ii) complexes are reported. These complexes consist of phenylisoquinoline, substituted phenylpyridines or tetrahydroquinolines as C^N cyclometalating ligands and dipivaloylmethane as an ancillary ligand. Depending on both the structure of the C^N cyclometalating ligands and the dopant concentration in the matrix, these platinum(ii) complexes exhibit different aggregation tendencies. This property affects the photoluminescence spectra of the investigated compounds and colour-stability of the fabricated OLEDs. Using the blue-green to yellow-green emitting complexes, the best results were obtained with the 2-(4- trifluoromethylphenyl)-5,6,7,8-tetrahydroquinoline based platinum(ii) complex. A maximum luminous efficiency of 4.88 cd A-1 and a power efficiency of 4.65 lm W-1, respectively, were achieved. Employing the red emitting phenylisoquinoline based complex as an emitter, colour-stable and efficient (4.71 cd A-1, 5.12 lm W-1) devices were obtained.
Oxygen and temperature sensitivity of blue to green to yellow light-emitting Pt(ii) complexes
Karakus, Cueneyt,Fischer, Lorenz H.,Schmeding, Sebastian,Hummel, Johanna,Risch, Nikolaus,Schaeferling, Michael,Holder, Elisabeth
experimental part, p. 9623 - 9632 (2012/08/28)
The synthesis and photophysical properties of a series of yellow-green to blue-green emitting heteroleptic, cyclometalated Pt(ii)(acac) complexes based on substituted phenylpyridine and tetrahydroquinoline ligands is reported. The luminescence intensities and lifetimes of these compounds were also studied in poly(styrene) films with respect to their responses to oxygen and temperature. Particularly, due to the insensitivity to oxygen quenching, these complexes are promising candidates as inert reference dyes in optical sensors. On the other hand, the Pt(ii) complex with 2-(4-bromophenyl)-5,6,7,8-tetrahydroquinoline as C^N ligand, displays a strong temperature quenching effect. The distinct response to temperature was additionally calibrated after incorporation in poly(vinylidene chloride-co-acrylonitrile) serving as oxygen-blocking matrix copolymer. The resulting yellow-green-emitting temperature sensor signifies an interesting alternative to the available mostly red emitting temperature-sensitive probes.
Synthesis of some Mannich bases with dimethylamine and their hydrazones and evaluation of their cytotoxicity against Jurkat cells
Kucukoglu, Kaan,Gul, Mustafa,Atalay, Mustafa,Mete, Ebru,Kazaz, Cavit,Hanninen, Osmo,Gul, Halise Inci
experimental part, p. 366 - 371 (2012/01/14)
1-Aryl-3-dimethylamino-1-propanone hydrochlorides type mono Mannich bases, D series, and corresponding hydrazone derivatives, K series, were synthesized and their cytotoxicity was tested against Jurkat cells (transformed human T-lymphocytes). The aryl part was changed as phenyl in D1 and K1, 4-methylphenyl in D2 and K2, 4-methoxyphenyl in D3 and K3, 4-hydroxyphenyl in D4 and K4, 4-chlorophenyl in D5 and K5, 3-methoxyphenyl in D6 and K6, 4-fluorophenyl in D7 and K7, 4-bromophenyl in D8 and K8, 3-hydroxyphenyl in D9 and K9, and 2-acetylthiophene in D10 and K10. Of the compounds synthesized, K2, K3, K5, K6, K7, K8, K9, and K10 are reported for the first time. Cytotoxic activities of the D and K series were compared with each other to see alterations in bioactivity depending on the chemical structures in Jurkat cells. Cytotoxicities of the compounds synthesized were also compared with the reference compound, 5-fluorouracil (CAS 148-82-3). Mono Mannich bases, D1 (3.60 times), D2 (4.45 times), D3 (2.46 times), D4 (3.52 times), D5 (5.18 times), D6 (3.20 times), D7 (3.23 times), D8 (3.95 times), D9 (3.36 times) and D10 (3.99 times) had 2.46-5.18 times higher cytotoxic potency than the reference compound 5-fluorouracil against Jurkat cells, while hydrazones K1 (4.92 times), K2 (4.65 times), K3 (6.04 times), K4 (6.34 times), K5 (4.67 times), K6 (5.12 times), K7 (5.39 times), K8 (8.31 times), K9 (4.65 times) and K10 (8.65 times) had 4.65-8.65 times higher cytotoxic potency than the reference compound 5-fluorouracil against the same cell line. On the other hand, hydrazone compounds K1 (1.37 times), K3 (2.46 times), K4 (1.80 times), K6 (1.60 times), K7 (1.67 times), K8 (2.11 times), K9 (1.38 times), and K10 (2.17 times) had 1.37-2.46 times higher cytotoxic potency than their corresponding mono Mannich bases. The results of this study suggest that hydrazones were better compounds compared with the corresponding mono Mannich bases in terms of cytotoxicity, and they may serve as model compounds to develop new cytotoxic agents for further studies. ECV ? Editio Cantor Verlag.
Synthesis of new 3-aryl-4,5-dihydropyrazole-1-carbothioamide derivatives. An investigation on their ability to inhibit monoamine oxidase
MacCioni,Alcaro,Orallo,Cardia,Distinto,Costa,Yanez,Sanna,Vigo,Meleddu,Secci
experimental part, p. 4490 - 4498 (2010/10/19)
Some differently substituted 3-aryl-4,5-dihydropyrazoles-1-carbothioamides have been synthesised with the aim to investigate their monoamine oxidase inhibitory activity. The chemical structures of the compounds have been characterized by means of their IR, 1H NMR, 13C NMR spectroscopic data and elemental analyses. All the active compounds showed a selective activity towards the B isoform of the enzyme, regardless of the substitution on the heterocyclic ring. The inhibition of the enzymatic activity was measured on human recombinant MAO isoforms, expressed in baculovirus infected BTI insect cells. Docking experiments were carried out with the aim to rationalize the mechanism of inhibition of the most active and selective compound.
Synthesis of some new 6-aryl-2-(3-oxo-1, 4-benzoxazin-6-yl)pyridines
Reddy,Reddy, Pragati,Reddy, G. Jagath,Rao, K. Srinivasa
, p. 135 - 138 (2007/10/03)
A series of some new 6-aryl-2-(3-oxo-1,4-benzoxazin-6-yl)pyridines (3a-g) have been prepared.
CARBOXAMIDE DERIVATIVES
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Page 17, (2008/06/13)
Compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein P, W, X, Y, R2, R3, r and s are as defined in the specification, processes for preparing such compounds, pharmaceutical compositions comprising such compounds and their use in therapy
Aryloxyphenylpropylamines their preparation and use
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, (2008/06/13)
Novel aryloxyphenylpropylamines having the formula STR1 wherein X is H, cyano, halogen, halogenoalkyl, C1-6 -alkoxy, C1-6 -alkyl, C1-5 -alkanoyl, C3-5 -alkylene, aryloxy or aralkoxy, and R is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C1-6 -alkyl, C1-6 -alkoxy, C1-6 -alkenyl, trifluoromethyl, C3-5 -alkylene, aryloxy or aralkoxy; and R1 and R2 independently is C1-10 -alkyl, C3-7 -cycloalkyl, C2-10 -alkenyl, C3-6 -cycloalkyl-C1-5 -alkyl, optionally substituted with C1-5 -alkoxy or cyano; R1 and R2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid, provided however that R1 is not C3-7 -cycloalkyl, C1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R2 is a methyl group. The novel compounds are useful in the treatment of anoxia, migraine, ischemia, epilepsy, traumatic injury and neurodegenerative diseases.
THE ELECTRONIC STRUCTURES OF INTRAMOLECULAR EXCIPLEXES WITH ALIPHATIC AMINES AS DONORS
Auweraer, M. van der,Vannerem, A.,Schryver, F. C. de
, p. 343 - 352 (2007/10/02)
Intramolecular exciplex formation between tertiary aliphatic amines and a phenyl group is investigated.The influences of the aliphatic chain length and para substitution of the phenyl moiety on the exciplex properties (fluorescence, rate constant, formati
