- PROCESS FOR THE SYNTHESIS OF ARYLDIAZONIUM SALTS USING NITROGEN OXIDES IN OXYGEN-CONTAINING GAS STREAMS, ESPECIALLY FROM INDUSTRIAL WASTE GASES
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The present invention relates to a process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases.
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Page/Page column 36; 37
(2017/06/30)
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- Synthesis and characterization of new pyrazole-based thiazoles
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A series of new 5-(heteroaryldiazenyl)thiazole incorporating pyrazole moiety have been synthesized through coupling of the thiazole with the appropriate heteroaryldiazonium salts. The newly synthesized compounds were characterized by elemental analysis, s
- Abdelhamid, Abdou O.,Gomha, Sobhi M.
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supporting information
p. 1409 - 1414
(2017/07/25)
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- Design, synthesis and anticancer activity of some novel 5-(4-methoxyphenyl)-2,4-dihydro-3H-pyrazol-3-one derivatives
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New pyrazole derivatives were designed and synthesized by the reaction of 5-(4-methoxyphenyl)-2,4-dihydro-3H-pyrazol-3-one (4) or 5-(4-methoxyphenyl)-2-phenyl-2,4-dihydro-3H-pyrazol-3-one (5) with series of aldehydes, substituted amines, isatins and phenylisothiocynate to yield 6a-j, 7a-k, 9a-d and 10a-b, respectively. The synthesized compounds were examined in vitro for their anti-tumor activities against HepG-2, PC-3 and HCT-116 human carcinoma cell lines using MTT assay. Eight compounds showed good anticancer activities against HCT-116 carcinoma cells and five compounds showed good anticancer activities against PC-3 cancer cells but all the compounds showed weak or no anticancer activities against HepG-2 liver cancer.
- Fathy, Usama,Gouhar, Rasha S.,Awad, Hanem M.
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p. 1427 - 1436
(2017/10/23)
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- Halobenzene cyanopyrazole compound containing purine structure as well as preparation method and application
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The invention discloses a halobenzene cyanopyrazole compound containing a purine structure as well as a preparation method and an application. The halobenzene cyanopyrazole compound is a compound with a general structure (I) as shown in the specification or a pharmaceutically acceptable salt thereof. The compound is low in dosage, good in insecticidal efficacy, simple in technique, low in cost and wide in market prospect.
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Paragraph 0105
(2016/10/31)
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- Flow synthesis of ethyl isocyanoacetate enabling the telescoped synthesis of 1,2,4-triazoles and pyrrolo-[1,2-c]pyrimidines
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The efficient flow synthesis of important heterocyclic building blocks based on the 1,2,4-triazole and pyrrolo[1,2-c]pyrimidine scaffold has been achieved. Crucially, a telescoped continuous flow process was developed based on the reaction of N-formylglycine with triphosgene to deliver a stream of ethyl isocyanoacetate in situ, which subsequently yielded the desired heterocyclic entities in a telescoped reaction. Additionally, the functionalisation of the pyrrolo[1,2-c]pyrimidine core via subsequent SEAr reactions was studied revealing insight into a 'halogen dance' phenomenon associated with these medicinally relevant architectures. This journal is
- Baumann, Marcus,Rodriguez Garcia, Antonio M.,Baxendale, Ian R.
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p. 4231 - 4239
(2015/04/14)
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- Synthesis, in vitro and in Silico studies of some novel 5-nitrofuran-2-yl hydrazones as antimicrobial and antitubercular agents
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In this study, we synthesized two series of novel 5-nitrofuran-2-carbohydrazides 21a-h and 22a-e in addition to a third series of thiophene-2-carbohydrazides 23a-g to develop potent antimicrobial and/or antitubercular agents. The newly synthesized compounds were evaluated in vitro for their antimicrobial and antimycobacterial activities. Most of the 5-nitrofuran-2-carbohydrazides 21a-h and 22a-e displayed variable activity against Aspergillus fumigates, Staphylococcus aureus, Streptococcus pneumonia, Bacillis subtilis, Salmonella typhimurium, Klebsiella pneumonia, Escherichia coli and Mycobacterium tuberculosis. The sulfonamide derivative 21f exhibited superior potency and broad-spectrum antimicrobial activity with minimum inhibitory concentration (MIC)=0.06-0.98 μg/mL and antimycobacterial activity with MIC=3.9 μg/mL. The 5-nitrofuran-2-carbohydrazides 21a, b, g, h and 22a-c exhibited significant antibacterial activity with MIC values in the range of 0.12-7.81 μg/mL. The significances of the 5-nitrofuran moiety and sulfonamide function were explored via the structure-activity relationship (SAR) study. In addition, docking studies revealed that the p-amino benzoic acid (PABA) and binding pockets of the dihydropteroate synthase (DHPS) were successfully occupied by compound 21f. Furthermore, two quantitative structure-activity relationship (QSAR) models were built to explore the structural requirements which controlled the activity.
- Abdel-Aziz, Hatem Abdel-Kader,Eldehna, Wagdy Mohamed,Fares, Mohamed,Elsaman, Tilal,Abdel-Aziz, Marwa Mostafa,Soliman, Dalia Hussein
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p. 1617 - 1630
(2015/11/24)
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- Design, synthesis and biological evaluation of small-azo-dyes as potent Vesicular Glutamate Transporters inhibitors
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Vesicular Glutamate Transporters (VGLUTs) allow the loading of presynapic glutamate vesicles and thus play a critical role in glutamatergic synaptic transmission. VGLUTs have proved to be involved in several major neuropathologies and directly correlated to clinical dementia in Alzheimer and Parkinson's disease. Accordingly VGLUT represent a key biological target or biomarker for neuropathology treatment or diagnostic. Yet, despite the pivotal role of VGLUTs, their pharmacology appears quite limited. Known competitive inhibitors are restricted to some dyes as Trypan Blue (TB) and glutamate mimics. This lack of pharmacological tools has heavily hampered VGLUT investigations. Here we report a rapid access to small molecules that combine benefits of TB and dicarboxylic quinolines (DCQs). Their ability to block vesicular glutamate uptake was evaluated. Several compounds displayed low micromolar inhibitory potency when size related compounds are thirty to forty times less potent (i.e. DCQ). We then confirmed the VGLUT selectivity by measuring the effect of the series on vesicular monoamine transport and on metabotropic glutamate receptor activity. These inhibitors are synthesized in only two steps and count among the best pharmacological tools for VGLUTs studies.
- Favre-Besse, Franck-Cyril,Poirel, Odile,Bersot, Tiphaine,Kim-Grellier, Elodie,Daumas, Stephanie,El Mestikawy, Salah,Acher, Francine C.,Pietrancosta, Nicolas
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p. 236 - 247
(2014/04/17)
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- Novel azo dyes derived from 8-methyl-4-hydroxyl-2-quinolone: Synthesis, UV-vis studies and biological activity
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In this study, N,N′-di-(2-methylphenyl)malonamide was synthesized and reacted with polyphosphoric acid to afford 8-methyl-4-hydroxyl-2-quinolone. Eight novel azo disperse dyes were then synthesized by linking diazotized p-substituted aniline derivatives w
- Moradi Rufchahi,Pouramir,Yazdanbakhsh,Yousefi,Bagheri,Rassa
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p. 425 - 428
(2013/07/11)
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- Di-substituted azocalix[4]arenes containing chromogenic groups: Synthesis, characterization, extraction, and thermal behavior
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In this study, the synthesis of chromogenic di-substituted azocalix[4]arene derivatives is described. Six novel azocalix[4]arenes (4a-f)were prepared by linking 4-methoxy, 4-methyl, 4-ethyl, 4-chloro, 4-bromo, and 4-nitroaniline to 25,26,27,28-tetrahydrox
- El?in, Serkan,Delig?z, Hasalettin
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p. 6832 - 6838
(2013/07/26)
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- Nanoparticles of organosilane-based nitrite ionic liquid immobilized on silica for the diazotization of aniline derivatives and subsequent synthesis of azo dyes
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Imidazolium based nitrite ionic liquid containing trimethoxysilyl group was prepared from the reaction of N-methylimidazole and (3-chloropropyl) trimethoxysilane. This ionic liquid was immobilized on silica covalently to give nanoparticles with the imidazolium nitrite moiety remaining intact. The diazotization reaction was performed as a model reaction to examine the activity of these nanoparticles as a nitrosonium source. Excellent performance was exhibited in the diazotization reaction of various aniline derivatives in the presence of HCl under mild heterogeneous conditions (room temperature and short reaction time). In-situ coupling of diazonium salts to a range of tertiary anilines, phenols and naphthols afforded the requisite azo dyes in good yield, using standard experimental procedures.
- Valizadeh, Hassan,Amiri, Mohammad,Hosseinzadeh, Fatemeh
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experimental part
p. 1308 - 1313
(2012/03/27)
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- Novel synthesis of hydrazide-hydrazone derivatives and their utilization in the synthesis of coumarin, pyridine, thiazole and thiophene derivatives with antitumor activity
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The reaction of cyanoacetyl hydrazine (1) with 3-acetylpyridine (2) gave the hydrazide-hydrazone derivative 3. The latter compound undergoes a series of heterocyclization reactions to give new heterocyclic compounds. The antitumor evaluation of the newly
- Mohareb, Rafat M.,Fleita, Daisy H.,Sakka, Ola K.
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experimental part
p. 16 - 27
(2011/03/23)
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- AMINO-HETEROARYL-CONTAINING PROKINETICIN 1 RECEPTOR ANTAGONISTS
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The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
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Page/Page column 52-53
(2009/06/27)
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- AZABICYCLO[3.1.0] HEXYLPHENYL DERIVATIVE AS MODULATORS OF DOPAMINE D3 RECEPTORS
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The present invention relates to novel compounds of formula (IA) or a salt thereof: Formula (IA), wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consis
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Page/Page column 34
(2008/06/13)
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- SPIRO-BENZIMIDAZOLES AS INHIBITORS OF GASTRIC ACID SECRETION
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The invention provides compounds of the formula (1), in which the substituents and symbols are as defined in the description. The compounds inhibit the secretion of gastric acid.
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Page/Page column 32
(2008/06/13)
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- NITROGENOUS FUSED-RING DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE DERIVATIVES, AND USE THEREOF AS DRUGS
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The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R 1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R 2 represent H, a halogen atom or an alkyl group; R 3 and R 4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc. ; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1)or(G-2) (in which E 1 represents H, F or OH; and E 2 represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.
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Page/Page column 36-37
(2010/11/24)
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- Synthesis and chemical reactivity of 3-oxo-2-arylhydrazono-propanenitriles
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2-Formyl-2-arylhydrazonoethanenitriles 6b-d where prepared via reacting enaminonitrile 2b,c with aromatic diazonium salts. These reacted with phenylhydrazine to yield bis hydrazones that were converted to arylazopyrazoles via a novel Vilsmeier-Haack reaction type. Reaction of 6c with hydroxylamine afforded oxime that could be successfully cyclised into arylazoisoxazole. Reaction of 6c with hydrazine hydrate to yield arylazoaminopyrazole that proved to be excellent precursors for synthesis functional substituted pyrazolopyrimidines.
- Abdallah, Sanaa O.,Metwally, Nadia H.,Anwar, Hany F.,Elnagdi, Mohamed H.
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p. 781 - 786
(2007/10/03)
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- INDOLIN PHENYLSULFONAMIDE DERIVATIVES
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The invention relates to novel substituted indolin phenylsulfonamide derivatives, to a method for the production thereof and to the use thereof in medicaments, especially as potent PPAR-delta activating compounds for the prophylaxis and/or treatment of cardiovascular diseases, especially dyslipidaemia and coronary heart diseases.
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Page/Page column 56; 57
(2010/11/30)
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- Synthesis, characterization and antimicrobial studies of some novel 3- arylazo-7-hydroxy-4-methylcoumarins
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A series of 3-arylazo-7-hydroxy-4-methylcoumarins have been synthesized in excellent yields (80-90%) and their structures established on the basis of IR, 1H NMR, mass spectral data and elemental analyses. Their purity has been ascertained by ch
- Sharma, Pratibha,Pritmani, Shreeya
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p. 1139 - 1142
(2007/10/03)
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- Reactions of 2-Arylhydrazones of 1,2,3-Triketones with 1,2-Diaminoethane. I. Synthesis and Spectral Characterization of 6-Arylazo-2,3-dihydro-1H-1,4-diazepines and 3,10-Diarylazo-4,9-dimethyl-5,8-diaza-3,9-dodecadiene-2,11-diones
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Reactions of 3-arylhydrazones of 2,3,4-pentanetrione (1a-1e) and 2-arylhydrazones of 1,3-diphenyl-1,2,3-propanetrione (1f-1l) with 1,2-diaminoethane have been studied.It was found, that 3-arylhydrazones of 2,3,4-pentanetrione react with 1,2-diaminoethane with formation of 6-arylazo-2,3-dihydro-1,4-diazepines (2a-2e) or the diarylazo derivatives of 4,9-dimethyl-5,8-diaza-3,9-dodecadiene-2,11-dione (3a-3e).Analogous reactions of 2-arylhydrazones of 1,3-diphenyl-1,2,3-propanetrione yielded exclusively the derivatives of dihydrodiazepine.The structure of obtained products has been elucidated on the basis of i.r., m.s. and 1H-n.m.r.spectra.
- Opozda, Ewa,Sledziewska, Ewa
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p. 601 - 606
(2007/10/02)
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- Antiimplantation Agents: Part I - 1-Arylthiosemicarbazides
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Several 1-arylthiosemicarbazides, 2-arylhydrazinothiazolines and 2-arylhydrazinodihydrothiazines have been examined for their antiimplantation activity in rats.Among the active compounds, 4-methyl-1-(3,5-bistrifluoromethylphenyl)thiosemicarbazide (3, C 2696-Go) and the corresponding 4,4-dimethyl (47), ethyl (4), n-butyl (5) and allyl (6) derivatives completely inhibit implantation at doses 10, 3, 20, 20 and 30 mg/kg respectively.The 3,4-dichlorophenyl analogue (32) is effective at a dose of 30 mg/kg. 2-(3,5-Bistrifluoromethylphenyl)hydrazinothiazoline (51) and the corresponding dihydrothiazine (63) show a weaker activity.The biological profile of C 2696-Go has been investigated in detail.It appears to prevent implantation by its antiuterotropic activity and ability to inhibit desiduoma formation.
- Nagarajan, K.,Talwalker, P.K.,Kulkarni, C.L.,Venkateswarlu, A.,Prabhu, S.S.,Nayak, G.V.
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p. 1243 - 1257
(2007/10/02)
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- Substituent Effects on 13C and 15N Chemical Shifts in Triazenes Studied by Principal Components Multivariate Data Analysis
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Principal components analysis was applied to the 13C and 15N chemical shift data on a series of fifteen 1-(para-substituted-phenyl)-3-acetyl-3-methyltriazenes.It was found that the halogen-substituted triazenes formed a class, based on substituent effects, which was different from the remaining eleven triazenes.A one-component model described the halogen class, whereas a two-component model was necessary for a description of the second class.In the second class, substituent tended to cluster to form groups depending on their electronic character.
- Dunn, III, W.J.,Lins, C.,Kumar, G.,Manimaran, T.,Grigoras, S.,et al.
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p. 450 - 456
(2007/10/02)
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- 1,2,3-Triazabutadienes. XIV. Investigations into the Acidic Cleavage of the Z-E-Isomeric 1-Aryl-3-- and 1-Aryl-3--triazenes
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The rate of the acid cleavage of the Z-E-isomeric 1-aryl-3-- and 1-aryl-3--triazenes 1 - 5 is investigated in dependence on the substituents in the aryl and benzo residue.The Z-isomer
- Fanghaenel, E.,Hohlfeld, J.
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p. 253 - 261
(2007/10/02)
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- Polarography of Some Arylazothiohydantoin Derivatives
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The polarographic behaviour of a series of arylazothiohydantoin derivatives has been investigated at a dropping mercury electrode.Two wawes were displayed.The first and predominant one is due to the reductive splitting of the azo-linkage by a 4e irreversi
- Darwish, S.,Fahmy, H. M.,Abdel Aziz, M. A.,El Maghraby, A. A.
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p. 344 - 349
(2007/10/02)
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