1798-83-0Relevant academic research and scientific papers
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 (2005)
A series of some new 6-aryl-2-(3-oxo-1,4-benzoxazin-6-yl)pyridines (3a-g) have been prepared.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 98, (2021/04/02)
The invention provides a composition of matter which: ? (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or ? (ii) consists of at least 90 % by weight of an atropisomer (2B) and 0-10 %
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.
A three-nitrogen azole compound of synthetic method (by machine translation)
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Paragraph 0021; 0022, (2017/09/29)
The invention discloses a three-nitrogen azole compounds 1 - 4 - chlorophenyl -3 - (1 H - 1, 2, 4 - triazole -1 - yl) -1 - propylamine synthetic method, to 4 - benzoyl chloride as the starting material, after coupling, condensation, oximation, reduction r
ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS
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Paragraph 0169, (2013/03/28)
Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
A novel antifungal agent with broad spectrum: 1-(4-Biphenylyl)-3-(1H- imidazol-1-yl)-1-propanone
Roman, Gheorghe,Mare?, Mihai,Nǎstasǎ, Valentin
, p. 110 - 118 (2013/04/10)
A series of (1-substituted aryl)-3-(1H-imidazol-1-yl)-1-propanones was synthesized through the N-alkylation of imidazole with 3-dimethylamino-1- (substituted aryl)-1-propanone hydrochlorides (ketonic Mannich bases). A second series of N1-substituted imidazoles was obtained by the reduction of the carbonyl function of the imidazole-ketones in the previous series by means of NaBH4. All of the compounds were evaluated for antifungal activity against 16 strains of Candida, and 3-(1H-imidazol-1-yl)-1-(4-biphenylyl)-1- propanone emerged as a broad-spectrum antifungal agent. Several 3-(1H-imidazol-1-yl)-1-(2′-(substituted benzyl)oxyphenyl)-1-propanones were also active towards Candida kefyr. Copyright
In vitro anti-Candida activity of certain new 3-(1H-Imidazol-1-yl)propan-1- one oxime esters
Attia, Mohamed I.,Zakaria, Azza S.,Almutairi, Maha S.,Ghoneim, Soraya W.
, p. 12208 - 12221 (2013/11/06)
Anti-Candida activities of certain new oximes 4a-d and their respective aromatic esters 5a-l are reported. The tested compounds 4a-d and 5a-l exhibited better anti-Candida profiles than fluconazole. Compound 5j, namely (E)-3-(1H-imidazol-1-yl)-1- phenylpropan-1-one O-4-chlorobenzoyl oxime emerged as the most active congener, with a MIC value of 0.0054 μmol/mL being more potent than both fluconazole (MIC > 1.6325 μmol/mL) and miconazole (MIC value = 0.0188 μmol/mL) as a new anti-Candida albicans agent.
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, structure characterization, and biological evaluation of some new 1,2,3-benzotriazole derivatives
Wan, Jun,Yan, Xia,Ma, Cuiping,Bi, Sai,Zhu, Hai-Liang
scheme or table, p. 970 - 983 (2011/12/04)
Ten novel benzotriazole compounds were synthesized. Their chemical structures were confirmed by 1H NMR, IR, and elemental analyses, coupled with three selected single-crystal structures (compounds A2, B3, and B5). Their antimycotic and antitumor activities were also investigated. The title compounds showed some antitumor activities, especially in the case of A3 and A4, which showed the most potent activity of propagation inhibition in liver and galactophore cancer cells. Birkhaueser Boston 2009.
SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
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Page/Page column 28, (2008/06/13)
This invention concerns sulfonylpyrazoline carboxamidine derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1), wherein the symbols have the meanings given in the description.
