Relevant articles and documents
All total 95 Articles be found
All total 95 Articles be found-
Doht,Haager
, p. 844,851,853 (1903)
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Synthesis of Certain New Thiazole and 1,3,4-Thiadiazole Derivatives via the Utility of 3-Acetylindole
Abdelhamid, Abdou O.,Gomha, Sobhi M.,Kandeel, Saher M.
, p. 1529 - 1536 (2017)
2-(2-(1-(1H-Indol-3-yl)ethylidene)-hydrazinyl)-4-substituted 5-(aryldiazenyl)thiazoles and 5-((1-(1H-indol-3-yl)ethylidene)hydrazono)-2-substituted-4-phenyl-4,5-dihydro-1,3,4-thiadiazoles were synthesized via reaction of hydrazonoyl halides and 2-(1-(1H-indol-3-yl)ethylidene)hydrazine-1-carbothioamide and alkyl 2-(1-(1H-indol-3-yl)ethylidene)hydrazine-1-carbodithioate in ethanolic triethylamine. Structures of the newly synthesis were elucidated on the basis of elemental analysis, spectral data, and alternative synthetic route whenever possible.
Synthesis, in vitro and in Silico studies of some novel 5-nitrofuran-2-yl hydrazones as antimicrobial and antitubercular agents
Abdel-Aziz, Hatem Abdel-Kader,Eldehna, Wagdy Mohamed,Fares, Mohamed,Elsaman, Tilal,Abdel-Aziz, Marwa Mostafa,Soliman, Dalia Hussein
, p. 1617 - 1630 (2015)
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.
Reaction of Triazene 1-Oxides: Novel Synthesis of Solid Arenediazonium Chlorides
Mohamed, Shaaban K.,Gomaa, Mohsen A.-M.,Nour El-Din, Ahmed M.
, p. 166 - 167 (1997)
Treatment of 1,3-diaryltriazene 1-oxides with oxalyl chloride in dry toluene at room temperature gives only solid arenediazonium chlorides; however, treatment with acetyl and benzoyl chlorides does not afford the corresponding diazonium chlorides.
Tetracyclic compounds from 1-oxo-1,2,3,4,5,6-hexahydrocycloocta[b]indole. Synthesis of oxazolo[4′5′:8,7]cycloocta[b]indoles
Vandana,Velumani,Prasad, K. J. Rajendra
, p. 299 - 306 (2003)
Japp-Klingmann method was used to diazotise aniline derivatives and 2-hydroxymethylenecyclooctanone 2 to obtain cyclooctan-1′,2′ -dione-1′-arylhydrazone 3 which upon acid cyclisation using kents reagent gave 1-oxo-1,2,3,4,5,6-hexahydrocycloocta[b]indole 4
New 2-pyrone-based hydrazones: Synthesis, spectral characterisation, UV–visible study and evaluation of the antiradicalar activity
Oukacha-Hikem, Djamila,Makhloufi-Chebli, Malika,Amar, Anissa,Bouherrou, Houria,Rachedi, Yahia,Meghezzi, Hacène,Silva, Artur M. S.,Hamdi, Maamar
, p. 590 - 598 (2017)
The synthesis of new 2-pyrone-based hydrazones has been prepared by the coupling of 6-methyl-2H-furo[3,2-c]pyran-3,4-dione with diazonium salts, obtained by diazotization of aniline derivatives. The structure of all compounds was established by spectrosco
Holt,Hopson-Hill
, p. 4251,4252 (1952)
ASYMMETRIC SYNTHESIS OF α-AMINO β-HYDROXY PHOSPHONIC ACIDS VIA BINAP-RUTHENIUM CATALYZED HYDROGENATION
Kitamura, Masato,Tokunaga, Makoto,Pham, Trang,Lubell, William D.,Noyori, Ryoji
, p. 5769 - 5772 (1995)
BINAP-Ru catalyzed hydrogenation of configurationally labile α-amido β-keto phosphonic esters gives the (R,R)- or (S,S)-α-amido β-hydroxy phosphonic esters in a highly enantio- and diastereoselective manner.
Electrochemical investigations of some newly synthesized arylazapyrazole derivatives
Arshad, Nasima,Ikramullah,Aamir, Muhammad,Sher, Muhammad
, p. 245 - 255 (2017)
Abstract: Three derivatives of arylazapyrazole ((E)-4-(phenyldiazenyl)-3,5-dimethyl-1H-pyrazole, (E)-4-[(4-fluorophenyl)diazenyl]-3,5-dimethyl-1H-pyrazole, and (E)-4-[(4-iodophenyl)diazenyl]-3,5-dimethyl-1H-pyrazole) were synthesized, characterized, and further investigated for their electrochemical behavior at glassy carbon electrode using cyclic voltammetry. All compounds were reduced following Ei Ci mechanism giving single cathodic peak in potential range 0 to ?2?V vs. Ag/AgCl. The plots of log iP vs. log ν showed that the electrode process is mixed adsorption-diffusion controlled. The kinetic parameters such as transfer coefficient (αn), diffusion coefficients (Do), and standard heterogeneous rate constants (ks) were determined from the electrochemical data. The values of Do were determined and found greater for the smallest among the three compounds. ks values were calculated by Laviron formalism which lies in the order of 10?2?s?1. Temperature and pH effects were studied and thermodynamic parameters such as change in free energy of activation (ΔG#), apparent activation energy (Ea), enthalpy (ΔH#), and entropy (ΔS#) of activation were determined. Negative values of Ea, ΔH#, and ΔS# imply that the electrode process needs lesser over potential with temperature rise, pre-adsorption of the analyte onto the electrode surface and the activated complex has a more organized structure than the reactants, respectively. Graphical abstract: [Figure not available: see fulltext.]
3-Aminopyrazolo[4,3-c]pyridine-4,6-dione as a precursor for novel pyrazolo[4,5,1-ij][1,6]naphthyridines and pyrido[4’,3’:3,4]pyrazolo[1,5-a]pyrimidines
Metwally, Nadia H.,Deeb, Emad A.
, p. 1614 - 1628 (2018)
The versatile, 3-aminopyrazolo[4,3-c]pyridine-4,6-dione (2) was synthesized and allowed to react with aldehydes, aryldiazonium chlorides, chalcones and enaminones to afford regioselectively the novel pyrazolo[4,3-c]pyridine derivatives 4a-c, pyrazolo[4,5,
Polymer complexes. LXX. Synthesis, spectroscopic studies, thermal properties and antimicrobial activity of metal(II) polymer complexes
Morgan, Sh. M.,El-Sonbati,El-Mogazy
, (2018)
The monomer 3-allyl-5-(phenylazo)-2-thioxothiazolidine-4-one (HL) was prepared by the reaction of allyl rhodanine with aniline through diazo-coupling reaction. Reaction of HL with Ni(II) or Co(II) salts gave polymer complexes (1–8) with general stoichiome
Rates and mechanisms of the thermal solvolytic decomposition of arenediazonium ions
Canning, Peter S. J.,McCrudden, Katharine,Maskill, Howard,Sexton, Brian
, p. 2735 - 2740 (1999)
Arenediazonium tetrafluoroborates have been prepared and the kinetics of solvolysis have been investigated in water, trifluoroethanol, water-trifluoroethanol mixtures, hexafluoropropan-2-ol, trifluoroacetic acid, and ethanol by a UV method. A heterolytic mechanism involving short-lived aryl cations leads to products derived from nucleophilic capture of the aryl cations by solvent or a solute. Ionic solutes in aqueous trifluoroethanol and trifluoromethoxybenzene in trifluoroethanol have no kinetic effect and neither does replacement of the tetrafluoroborate counter-ion by chloride in trifluoroethanol. Rate constants for any one compound are not very solvent dependent, the reactions generally being characterised by high enthalpies of activation and appreciably positive entropies of activation. Compounds with 4-Cl, 4-F, 4-NO2, and 4-MeO substituents proved too unreactive for kinetic studies, but for different reasons. In ethanol, a radical reaction with characteristically different activation parameters competes with the heterolytic path and leads to hydrodediazoniation (reduction) by hydrogen atom abstraction from the CH2 group of ethanol.
New Thiophene Derivatives as Antimicrobial Agents
Mabkhot, Yahia Nasser,Kaal, Nahed Ahmed,Alterary, Seham,Mubarak, Mohammad S.,Alsayari, Abdulrhman,Bin Muhsinah, Abdullatif
, p. 2845 - 2953 (2019)
Phenacylbromide derivatives constitute a multilateral group of precursors for the synthesis of numerous heterocycles of organic compounds. Briefly, 5-(2-bromo-acetyl)-substituted-thiophene derivative has been used as a synthon for synthesis of new thiophene-containing compounds through the reaction with nucleophilic nitrogen compounds and thioamides. The suggested structures of the newly synthesized thiophene compounds were confirmed and assured with different spectroscopic tools and with CHN elemental analysis. Additionally, the antimicrobial activity of these thiophene compounds was recorded to investigate their potency against various types of bacteria and fungi. Results showed that these compounds exhibit significant inhibitory activity against the growth of tested bacterial and fungal strains and that some derivatives were more potent than the employed reference drugs.
Holt,Bullock
, p. 2310 (1950)
Synthesis and antimicrobial activity of substituted 4-aryl-3-phenylhydrazono-2,4-dioxobutanoic acids
Pimenova,Khamatgaleev,Voronina,Andreichikov
, p. 424 - 426 (1999)
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Ligand-free Suzuki-Miyaura cross-coupling reactions of aryltriazenes with arylboronic acids
Nan, Guangming,Zhu, Fanghua,Wei, Zhijun
, p. 72 - 78 (2011)
The boron trifluoride induced Suzuki-Miyaura cross-coupling of aryltriazenes with arylboronic acids catalyzed by Pd(OAc)2 without added ligands has been achieved for the first time. The reactions performed at room temperature under an argon atmosphere give biaryls in good to excellent yields. It is noteworthy that the reactions were conducted under mild and ligand-free conditions. The boron trifluoride induced Suzuki-Miyaura cross-coupling of aryltriazenes with arylboronic acids catalyzed by Pd(OAc) 2 without added ligands has been achieved for the first time. Copyright
Selective Formation of Products of Interrupted Feist-Benary Reaction under the Conditions of Hantzsch Pyrrole Synthesis
Matiichuk,Frolov,Pokhodylo,Pavlyuk,Obushak
, p. 799 - 801 (2018)
Reaction of 3-aryl-2-chloropropanal with 1-arylsulfonylpropan-2-ones in aqueous ammonia and alcohol under the conditions of Hantzsch pyrrole synthesis led to the selective formation of the products of interrupted Feist-Benary reaction, 2-(R-benzyl)-4-aryl
Facile Synthesis of Pyrazolo[3,4-c]pyrazoles Bearing Coumarine Ring as Anticancer Agents
Gomha, Sobhi M.,Abdel-aziz, Hassan M.,El-Reedy, Ahmed A. M.
, p. 1960 - 1965 (2018)
In the present study, 2-(2-oxo-2H-chromene-3-carbonyl)-5-phenyl-2,4-dihydro-3H-pyrazol-3-one was prepared and reacted with various hydrazonoyl halides to give a series of 2-(2-oxo-2H-chromene-3-carbonyl)-5-phenyl-4-((2-phenylhydrazono)methyl)-2,4-dihydro-3H-pyrazol-3-one in good yield. Cyclization of the latter hydrazone with POCl3 yielded the respective 3-(3-phenyl- 4,6-disubstituted-1,6-dihydropyrazolo[3,4-c]pyrazole-1-carbonyl)-2H-chromen-2-ones. The structures of the newly synthesized compounds were established on the basis of spectroscopic evidences and their alternative syntheses. The newly synthesized compounds were evaluated for their antitumor activities against hepatocellular carcinoma (HepG2) cell line and the results revealed promising activities of compounds 4e, 4c, and 4d with IC50 equal 0.92?±?0.22, 1.43?±?0.19, and 2.17?±?0.21?μM, respectively.
Design, synthesis, and molecular docking study of novel heterocycles incorporating 1,3,4-thiadiazole moiety as potential antimicrobial and anticancer agents
El-Naggar, Mohamed,Sallam, Hanan A.,Shaban, Safaa S.,Abdel-Wahab, Salwa S.,Amr, Abd El-Galil E.,Azab, Mohammad E.,Nossier, Eman S.,Al-Omar, Mohamed A.
, (2019)
A new series of 5-(3,5-dinitrophenyl)-1,3,4-thiadiazole derivatives were prepared and evaluated for their in vitro antimicrobial, antitumor, and DHFR inhibition activity. Compounds 9, 10, 13, and 16 showed strong and broad-spectrum antimicrobial activity comparable to Amoxicillin and Fluconazole as positive antibiotic and antifungal controls, respectively. Compounds 6, 14, and 15 exhibited antitumor activity against four human cancer cell lines, CCRF-CEM leukemia, HCT-15 colon, PC-3 prostate, and UACC-257 melanoma cell lines using Doxorubicin as a reference drug. Compounds 10, 13, 14, and 15 proved to be the most active DHFR inhibitors with an IC50 range of 0.04 ± 0.82–1.00 ± 0.85 μM, in comparison with Methotrexate (IC50 = 0.14 ± 1.38 μM). The highly potent DHFR inhibitors shared a similar molecular docking mode and made a critical hydrogen bond and arene?arene interactions via Ser59 and Phe31 amino acid residues, respectively.
A Novel Synthesis of Some 1,4-Phenylene-bis-heterocyclic Derivatives and of Some Pyran, Pyrano[2,3-c]pyrazole, and Pyrano[2,3-d]pyrimidine Derivatives [1]
Abdelrazek,Helal,Hebishy,Hassan
, p. 1026 - 1031 (2015)
p-Diacetyl benzene 1 undergoes bromination to afford p-bromoacetyl phenacyl bromide 2. Compound 2 reacts with twofold excess of malononitrile to afford 2-{2-[4-(3,3-Dicyanopropionyl)-phenyl]-2-oxo-ethyl}-malononitrile 3. Compound 3 could be cyclized to af
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Kidd
, p. 198,205-207 (1937)
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A comprehensive spectroscopic, solvatochromic and photochemical analysis of 5-hydroxyquinoline and 8-hydroxyquinoline mono-azo dyes
Coelho, Paulo J.,Lup, Andrew Ng Kay,Mahon, Peter J.,Pesyan, Nader Noroozi,Ramezanitaghartapeh, Mohammad,Raposo, M. Manuela M.,Rashidnejad, Hamid,Soltani, Alireza
, (2020/10/06)
A series of novel substituted-azo dyes 8-(aryldiazenyl)quinolin-5-ol (5a-i) were synthesized by the coupling reaction of 5-hydroxyquinoline with diazotized aniline derivatives in the presence of NaNO2 in HCl/H2O mixture. The study of
Preparation method of monocyclic or polycyclic compound containing pyrrole ring
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Paragraph 0028-0030; 0031-0032, (2021/05/15)
The invention discloses a preparation method of a monocyclic or polycyclic compound containing a pyrrole ring. An enamine compound is used as a raw material and is continuously subjected to diazotization, reduction and cyclization synthesis with a carbony
INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASE
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Paragraph 0518-0520, (2021/05/29)
Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
Synthetic method for preparing 5-aminobenzimidazolone
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Paragraph 0016; 0031-0033; 0042-0044, (2021/07/17)
The invention discloses a synthesis method for preparing 5-aminobenzimidazolone (TM), which comprises the following steps: firstly, carrying out diazotization reaction on aniline to prepare aniline diazonium salt; secondly, coupling the aniline diazonium salt with o-phenylenediamine to generate an azo compound, and carrying out a reaction on the azo compound and urea under the catalysis of concentrated sulfuric acid to generate an azobenzimidazolone compound, and subjecting the azobenzimidazolone compound to a hydrogenation reduction reaction to obtain the target compound 5-aminobenzimidazolone. The method disclosed by the invention is simple in process, high in selectivity and high in product yield, all used reactants are utilized, and the method has very high atom economy. The use of a nitration reagent concentrated nitric acid is avoided, the wastewater and the generation of salt in the wastewater are greatly reduced, and the method is a green production process. In addition, the hydrocracking reduction operation is simple, no other iron mud such as iron powder reduction is generated, no waste residue is basically generated, the quality of a finished product is obviously improved, filter-pressing rinsing water can be repeatedly used for more than multiple times, the cost is reduced, and the environmental pollution is reduced.
Uses of ethyl benzoylacetate for the synthesis of thiophene, thiazole, pyridine, and pyran derivatives with antitumor activities
Mohareb, Rafat M.,Mostafa, Bahaa M.
, (2020/01/22)
The reaction of ethyl benzoylacetate with malononitrile in an oil bath at 120°C gave the condensation product 3. The latter compound underwent a series of heterocyclization to give thiophene, thiazole, pyridine, and pyran derivatives. The structures of the synthesized products were established on the basis of analytical and spectral data. The antitumor evaluation of the newly synthesized products against the six cancer cell lines namely human gastric cancer (NUGC and HR), human colon cancer (DLD1), human liver cancer (HA22T and HEPG2), human breast cancer (MCF), nasopharyngeal carcinoma (HONE1), and normal fibroblast cells (WI38) indicated that many compounds expressed high inhibition against the six cancer cell lines. Compounds 3, 8a, 8c, 14b, 16b, 16c, 16d, 19a, 19b, 20a, 22a, 27b, and 28a were the most cytotoxic compounds among the tested compounds.
