- Synthesis, antiviral, antituberculostic, and antibacterial activities of some novel, 4-(4-substituted phenyl)-6-(4-nitrophenyl)-2-(substituted imino)pyrimidines
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A variety of novel 4-(4-substituted phenyl)-6-(4-nitrophenyl)-2-substituted imino) pyrimidines were synthesized by reacting 4-(4-substituted phenyl)-6-(4-nitrophenyl)-2-amino pyrimidines with different substituted aromatic aldehydes, coumarin chloroisatin
- Siddiqui, Anees A.,Rajesh, Ramadoss,Mojahid-Ul-Islam,Alagarsamy, Veerachamy,De Clercq, Erick
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- Synthesis of chalcone derivatives by phthalhydrazide-functionalized tio2-coated nano-fe3o4 as a new heterogeneous catalyst
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Phthalhydrazide immobilized on TiO2-coated nano Fe3O4 (Fe3O4-P) was synthesized and characterized by FT-IR, XRD, SEM, EDS and VSM analysis. The resulting magnetic nanocatalyst was used as a catalyst for the synthesis of chalcone derivatives which affords the desired products in good to excellent yields. This catalyst can be isolated readily after completion of the reaction by an external magnetite field and reused several times without significant loss of activity.
- Farahi, Mahnaz,Karami, Bahador,Keshavarz, Raziyeh,Nia, Forough Motamedi
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p. 407 - 414
(2021/09/07)
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- ADME properties, bioactivity and molecular docking studies of 4-amino-chalcone derivatives: new analogues for the treatment of Alzheimer, glaucoma and epileptic diseases
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In this study, in vitro inhibition effects of (E)-1-(4-aminophenyl)-3-(aryl) prop-2-en-1-one (4-amino-chalcones) derivatives (3a–o) on acetylcholinesterase (AChE) enzyme and human erythrocyte carbonic anhydrase I and II isoenzymes (hCA I- II) were investigated. And also, the biological activities of 4-amino-chalcone derivatives against enzymes which names are acetylcholinesterase (PDB ID: 1OCE), human Carbonic Anhydrase I (PDB ID: 2CAB), human carbonic anhydrase II (PDB ID: 3DC3), were compared. After the results obtained, ADME/T analysis was performed in order to use 4-amino-chalcone derivatives as a drug in the future. Effective inhibitors of carbonic anhydrase I and II isozymes (hCAI and II) and acetylcholinesterase (AChE) enzymes with Ki values in the range of 2.55 ± 0.35–11.75 ± 3.57?nM for hCA I, 4.31 ± 0.78–17.55 ± 5.86?nM for hCA II and 96.01 ± 25.34–1411.41 ± 32.88?nM for AChE, respectively, were the 4-amino-chalcone derivatives (3a–o) molecules.
- Gürdere, Meliha Burcu,Budak, Yakup,Kocyigit, Umit M.,Taslimi, Parham,Tüzün, Burak,Ceylan, Mustafa
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- Three Step Synthesis of Fully and Differently Arylated Pyridines
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Condensation of β-(2-pyridyl)enamine and α,β-unsaturated ketone in the presence of FeCl3 under air afforded highly substituted pyridines. In this transformation, FeCl3 acted as not only an acid catalyst but also an oxidant for the in
- Arita, Mao,Yokoyama, Soichi,Asahara, Haruyasu,Nishiwaki, Nagatoshi
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p. 466 - 474
(2020/01/25)
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- 2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors
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A novel 2-thiopyrimidine/chalcone hybrid was designed, synthesised, and evaluated for their cytotoxic activities against three different cell lines, K-562, MCF-7, and HT-29. The most active cytotoxic derivatives were 9d, 9f, 9n, and 9p (IC50=0.77–1.74 μM, against K-562 cell line), 9a and 9r (IC50=1.37–3.56 μM against MCF-7 cell line), and 9a, 9l, and 9n (IC50=2.10 and 2.37 μM against HT-29 cell line). Compounds 9a, 9d, 9f, 9n, and 9r were further evaluated for their cytotoxicity against normal fibroblast cell line WI38. Moreover, STAT3 and STAT5a inhibitory activities were determined for the most active derivatives 9a, 9d, 9f, 9n, and 9r. Dual inhibitory activity was observed in compound 9n (IC50=113.31 and 50.75 μM, against STAT3 and STAT5a, respectively). Prediction of physicochemical properties, drug likeness score, pharmacokinetic and toxic properties was detected.
- Lamie, Phoebe F.,Philoppes, John N.
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p. 864 - 879
(2020/04/07)
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- Rapid abnormal [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles with chalcones
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The rapid synthesis of novel dicyclic spiropyrrolidine was reported, using [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles, generated from the condensation of substituted isatins and pyrazolidones, with chalcones in 2-5 min. The dicy
- Yue, Guizhou,Dou, Zhengjie,Zhou, Zexi,Zhang, Li,Feng, Juhua,Chen, Huabao,Yin, Zhongqiong,Song, Xu,Liang, Xiaoxia,Wang, Xianxiang,Rao, Hanbing,Lu, Cuifen
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supporting information
p. 8813 - 8817
(2020/06/08)
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- Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives
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Novel enamine derivatives were synthesized from the reaction of lactone and chalcones and their antiproliferative and cytotoxic activities against six cancer cell lines (e. g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell lines (e. g., FL) were investigated along with their mode of interactions with CT-DNA. Most of the enamine derivatives with IC50 values of 86–168 μM demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5-fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (~6 nm), indicating that they bind to the DNA by way of an intercalative or minor groove binding mode. The binding constants of the compounds are in the range of 0.1×103 M?1–2.3×104 M?1. The antiproliferative activity of studied enamine derivatives could possibly be due to their DNA binding as well as their cytotoxic properties. In addition to these assays, the chalcones and enamine derivatives were investigated by molecular docking to calculate the synergistic effect of antiproliferative activities against six human cancer cell lines.
- Burcu Gürdere, Meliha,Aydin, Ali,Yencilek, Belk?z,Ertürk, Fatih,?zbek, O?uz,Erkan, Sultan,Budak, Yakup,Ceylan, Mustafa
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- Indium(III) triflate-catalyzed reactions of AZA-michael adducts of chalcones with aromatic amines: Retro-michael addition versus quinoline formation
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The indium(III) triflate-catalyzed reaction of aza-Michael adducts of chalcones with aromatic amines has been investigated. The Michael adducts derived from substituted anilines and chalcones underwent retro-Michael addition to give the original starting materials, whereas the adducts derived from 1-naphthylamines and chalcones afforded quinolines. A six-membered cyclic transition state has been proposed to explain the retro-Michael addition, while a Povarov mechanism has been put forward to explain the quinoline formation.
- Selvi, Thangavel,Velmathi, Sivan
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p. 4087 - 4091
(2018/04/14)
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- Method for preparing chalcone compound
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The invention relates to a method for preparing a chalcone compound. The method utilizes organic solutions of acetophenone or its derivative and benzyl alcohol or its derivative as reaction substrates and a metallic oxide as a catalyst to prepare the chalcone compound through oxidative condensation. The method comprises mixing acetophenone or its derivative, benzyl alcohol or its derivative and the metallic oxide in an organic solvent, putting the mixture into a pressure container, sealing the pressure container, stirring the mixture at a temperature of 40-150 DEG C for 0.5-24h and separating the reaction product to obtain the chalcone compound. The method has the advantages of easy separation of the product from the catalyst, catalyst recycle, simple reaction process and operation easiness and has a chalcone yield of 66%.
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Paragraph 0084-0085
(2017/02/28)
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- Synthesis, cyclooxygenase inhibition and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing methanesulphonyl pharmacophore
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A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives 13a–p were synthesized via aldol condensation of 3/4-nitroacetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine hydrochloride. All the synthesized compounds were evaluated for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. All compounds were more potent inhibitors for COX-2 than COX-1. While most compounds showed good anti-inflammatory activity, compounds 13d, 13f, 13k and 13o were the most potent derivatives (ED50 = 66.5, 73.4, 79.8 and 70.5 μmol/kg, respectively) in comparison with celecoxib (ED50 = 68.1 μmol/kg). Compounds 13d, 13f, 13k and 13o (ulcer index = 3.89, 4.86, 4.96 and 3.92, respectively) were 4–6 folds less ulcerogenic than aspirin (ulcer index = 22.75) and showed approximately ulceration effect similar to celecoxib (ulcer index = 3.35). In addition, molecular docking studies were performed for compounds 13d, 13f, 13k and 13o inside COX-2 active site which showed acceptable binding interactions (affinity in kcal/mol ?2.1774, ?6.9498) in comparison with celecoxib (affinity in kcal/mol ?6.5330).
- Abdellatif, Khaled R. A.,Elsaady, Mohammed T.,Abdel-Aziz, Salah A.,Abusabaa, Ahmed H. A.
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p. 1545 - 1555
(2016/10/09)
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- Synthesis of some novel 5,7-disubstituted-2-phenyl-5H-[1,3,4]thiadiazolo [3,2-a]pyrimidine derivatives and evaluation of their biological activity
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Background: In the present study, a series of 5,7-disubstituted-2-phenyl-5H-[1,3,4] thiadiazolo[3,2-a]pyrimidine derivatives have been reported. The title compounds were synthesized by the reaction of substituted chalcones with 5-phenyl-1,3,4-thiadiazol-2-amine in n-butanol. Methods: All reactions were performed at reflux temperature and the synthesized compounds were characterized by IR, NMR and Mass spectroscopic techniques. Results: The synthesized compounds were screened for their antimicrobial and antioxidant activities. The compounds displayed significant antimicrobial and antioxidant activities. Additionally, the selected compounds were screened for in silico molecular docking studies. Conclusion: In the present work, we have reported an efficient method for the synthesis of some new 5,7-disubstituted-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidine derivatives. Collectively, all the current computational insights support the in vitro observations seen for antimicrobial and antioxidant agents. Further, the pyrimidine derivatives might act as potential specific inhibitors of G6P synthase thereby facilitating its biological activities. From the activity results, it has been concluded that among the studied compounds, compounds 5b, 5d, 5e, 5g, 5i, 5m and 5n could serve as potential antimicrobial and antioxidant agents.
- Venkatesh, Talavara,Bodke, Yadav D.,Joy, Nibin M.,Vinoda,Shiralgi, Yallappa,Dhananjaya
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p. 661 - 671
(2017/01/13)
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- Inhibitory potential of some chalcones on cathepsins B, H and L
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Cathepsins, intracellular proteases, are known to be involved in a number of physiological processes such as degradation of extracellular proteins, prohormone processing, progressions of atherosclerosis etc. High levels of cathepsins have also been indica
- Garg, Shweta,Raghav, Neera
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p. 72937 - 72949
(2015/09/15)
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- Efficient synthesis of 2,4-diaryl hexahydroquinoline-5-one derivatives in the presence of triethylamine
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Abstract A convenient and efficient protocol for the synthesis of 2,4-diaryl hexahydroquinoline-5-one derivatives has been accomplished by a three-component reaction of 1,3-diaryl-2-propen-1-ones, dimedone and ammonium acetate catalyzed by triethylamine under solvent-free conditions. The simple experimental procedure, use of an inexpensive catalyst, short reaction times, and excellent yields make this procedure facile, practical, and sustainable.
- Karimi-Jaberi, Zahed,Azadi, Maryam
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p. 6741 - 6747
(2015/02/19)
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- Synthesis and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing an aminosulphonyl pharmacophore
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A novel series of 2-pyrazoline derivatives 13a-l was synthesized via aldol condensation of 4-substituted acetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-hydrazinobenzenesulfonamide hydrochlorid
- Abdellatif, Khaled R. A.,Abdelgawad, Mohamed A.,Elshemy, Heba A. H.,Alsayed, Shahinda S. R.,Kamel, Gehan
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p. 1932 - 1942
(2015/11/24)
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- One-pot synthesis of chalcone epoxides - A green chemistry strategy
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Waste minimization is a very important aspect of an environmentally benign protocol. A one-pot consecutive process has been developed for chalcone epoxide synthesis that allows compounds to be prepared without having to isolate and purify the intermediates. The strategy utilizes consecutive Claisen Schmidt condensation and epoxidation reactions to prepare chalcone epoxides from substituted benzaldehydes and acetophenones in good yields.
- Ngo, Dalyna,Kalala, Mbelu,Hogan, Victoria,Manchanayakage, Renuka
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p. 4496 - 4500
(2014/08/05)
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- Amberlyst-15 and Amberlite-200C: Efficient catalysts for aldol and cross-aldol condensation under ultrasound irradiation
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This paper presents an improved synthesis of trans-chalcones and α,α′-bis(arylmethylidene) cycloalkanones under ultrasound irradiation in the presence of commercial acid-resins as catalysts in solvent free conditions. Several trans-chalcones and α,α′- bis(arylmethylidene) cycloalkanones were synthesized in good yields and excellent selectivity in a short reaction time.
- Lahyani, Achraf,Chtourou, Manef,Frikha, Mohamed Hédi,Trabelsi, Mahmoud
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p. 1296 - 1301
(2013/06/27)
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- Synthetic chalcone derivatives as inhibitors of cathepsins K and B, and their cytotoxic evaluation
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A series of chalcone derivatives, 1-15, were prepared by Claisen-Schmidt condensation and evaluated for their cytotoxicities on tumor cell lines and also against proteolytic enzymes such as cathepsins B and K. Of the compounds synthesized, (E)-3-(3,4-dimethoxyphenyl)-1-phenylprop-2-en-1-one (12), (E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one (13), (E)-3-(4-methoxyphenyl)-1- phenylprop-2-en-1-one (14), and (E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one (15) showed significant cytotoxicities. The most effective compound was 15, which showed high cytotoxic activity with an IC50 value lower than 1 μg/ml, and no selectivity on the tumor cells evaluated. Substituents at C(4) of ring B were found to be essential for cytotoxicity. In addition, it was also demonstrated that some of these chalcones are moderate inhibitors of cathepsin K and have no activity against cathepsin B. Copyright
- Ramalho, Suelem Demuner,Bernades, Aline,Demetrius, Giulio,Noda-Perez, Caridad,Vieira, Paulo Cezar,Dos Santos, Caio Yu,Da Silva, James Almada,De Moraes, Manoel Odorico,Mousinho, Kristiana Cerqueira
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p. 1999 - 2006
(2013/12/04)
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- Synthesis, antitubercular activity, and QSAR analysis of substituted nitroaryl analogs: Chalcone, pyrazole, isoxazole, and pyrimidines
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In the present investigation, 4-nitroacetophenone, on condensation with appropriate aldehydes in ethanolic sodium hydroxide solution, yielded the corresponding chalcones. These corresponding chalcones were reacted with hydrazine hydrate, urea, thiourea, a
- Gupta, Revathi A.,Kaskhedikar, Satish G.
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p. 3863 - 3880
(2013/07/26)
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- Synthesis, characterization, and anti-amoebic activity of N-(pyrimidin-2-yl)benzenesulfonamide derivatives
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A new series of N-(pyrimidin-2-yl)benzenesulfonamide derivatives, 3a-3i and 4a-4i, was synthesized from pyrimidin-2-amines, 2a-2i, with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds
- Roouf Bhat, Abdul,Arshad, Mohammad,Ju Lee, Eun,Pokharel, Smritee,Choi, Inho,Athar, Fareeda
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p. 2267 - 2277
(2014/01/06)
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- Synthesis, characterization and fluorescence studies of 3,5-diaryl substituted 2-pyrazolines
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A series of 2-pyrazolines have been synthesized from α, β unsaturated ketones and hydrazine hydrate with acetic/formic acid in ethanol/DMSO. The structures of 2-pyrazolines have been established by spectroscopic techniques i.e. UV, IR, 1H NMR, 13C NMR and micro element analysis. Fluorescence spectra were recorded in the solution at fixed concentration and same excitation wavelength at 290 nm. The absorption band positions of all the compounds broadly lie between 280 and 336 nm and fluorescence band positions in the range between 300 and 370 nm, the near ultraviolet region.
- Nee Pant, Geeta Joshi,Singh, Pramod,Rawat,Rawat,Joshi
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scheme or table
p. 1075 - 1079
(2011/04/16)
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- Efficient synthesis of chalcone derivatives catalyzed by re-usable hydroxyapatite
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Hydroxyapatite was found to be a very efficient heterogeneous catalyst for the preparation of chalcone derivatives via Claisen-Schmidt condensation using microwave irradiation. The impact of water on the catalyst reactivity was studied and was thought to act as co-catalyst due to the high activation observed in its presence. To investigate the origin of this activation, different organic solvents of similar or higher microwave absorbance as/to water were also tested, and it was confirmed that water is acting as co-catalyst when combined with hydroxyapatite, making the process highly efficient. The catalyst was easily recovered and efficiently re-used.
- Solhy,Tahir,Sebti,Skouta,Bousmina,Zahouily,Larzek
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experimental part
p. 189 - 193
(2010/11/04)
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- Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: Synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone
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We have examined the antimalarial structure-activity relationship of a series of methoxylated chalcones (A-CHCH-CO-B) against Plasmodium falciparum (3D7 strain) using fluorescence-based SYBR Green assay. Our study has revealed that electron releasing methoxy groups on ring A and electron withdrawing groups on ring B increases antimalarial potency while the positional interchange of these groups causes a decrease. In particular, 2,4,5-trimethoxy substitution pattern at ring A provided potent analogues which were easily derived from abundantly available natural β-asarone rich Acorus calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC50: 1.8 μM) and 26 (IC50: 2 μM) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.
- Kumar, Rakesh,Mohanakrishnan, Dinesh,Sharma, Abhishek,Kaushik, Naveen Kumar,Kalia, Kalpana,Sinha, Arun Kumar,Sahal, Dinkar
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experimental part
p. 5292 - 5301
(2011/02/23)
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- Synthesis and antimicrobial activity of some pyrazoline derivatives
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The objective of present study is to synthesize and screening of antimicrobial activity of some derivatives of pyrazoline. 1H-[4-nitro phenyl-5-(substituted phenyl)]pyrazoline has been used as a precursor to synthesize some biologically active heterocycles. Reaction of 1-(4-nitrophenyl)-3-(substituted phenyl) prop-2-en-1-one with hydrazine hydrate gave 1H-(3-nitrophenyl-5-(substituted phenyl) pyrazoline which on reaction with benzoyl chloride in pyridine gave 1-benzoyl-(4-nitrophenyl)-5-(substituted phenyl) prazoline and on reaction with acetic acid yields 1-acetyl-(4- nitrophenyl)-5-(substituted phenyl) pyrazoline derivatives. Several derivatives have been synthesized and screened for their antimicrobial efficacy against Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae. Antifungal activity against, Aspergillus flavus, Fusarium oxisporum, Aspergillus niger and Trichoderma viridae.
- Ahirwar,Gautam,Shrivastava
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experimental part
p. 5297 - 5302
(2012/07/28)
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- A new lewis acid system palladium/TMSCl for Catalytic aldol condensation of aldehydes with ketones
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Palladium on charcoal effectively catalyzed the aldol condensation reactions of different ketones with aldehydes in the presence of trimethylsilyl chloride (TMSCl). The following reactions were investigated: (1) aromatic aldehydes with cycloalkanones, (2) aromatic aldehydes with aromatic ketones, (3) cycloalkanones with aliphatic aldehydes, and (4) the self-condensation reactions of aliphatic aldehydes and cycloalkanones.
- Zhu, Yulin,Pan, Yuanjiang
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p. 668 - 669
(2007/10/03)
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- Application of natural phosphate modified with sodium nitrate in the synthesis of chalcones: A soft and clean method
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The solid obtained by impregnation of natural phosphate (NP) with a solution of sodium nitrate, followed by calcination at 900°C, is a strongly basic catalyst that is easily prepared from cheap precursors. The catalytic activity of this solid in the Claisen-Schmidt condensation was studied and high yields were obtained with small amounts of catalyst. The reaction rate depends on the substitution in both benzaldehyde and acetophenone derivatives. The effect of the solvent, as well as the addition of water and ammonium salt, was investigated as well. The catalyst can be easily recovered and efficiently reused.
- Sebti, Said,Solhy, Abderrahim,Tahir, Rachid,Abdelatif, Smahi,Boulaajaj, Said,Mayoral, Jose A.,Garcia, Jose I.,Fraile, Jose M.,Kossir, Abdelali,Oumimoun, Hammou
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- Multiple substituent effects on 13C chemical shifts in phenylstyryl ketones: Applicability of interactive free energy relationship
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13C chemical shifts for 23 mono- and di-substituted phenyl styryl ketones have been determined. The shieldings and deshieldings are compared with previous results for other aromatic derivatives. Correlations of the 13C chemical shifts of vinyl carbons with Hammett σ parameters has been determined to provide a consistent picture of electronic effects transmitted through the carbon framework of the compounds studied. Slopes obtained from such Hammett's plots are termed as ρ, and using these 'ρ' values applicability of interactive free energy relationship to chemical shift values has been tested. The cross- interaction constants qx and qy values for C-α are found to be -1.02 and -1.20 and for C-β are -1.46 and -1.19.
- Annapoorna,Prasad Rao,Sethuram
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p. 1341 - 1345
(2007/10/03)
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- Calcined sodium nitrate/natural phosphate: An extremely active catalyst for the easy synthesis of chalcones in heterogeneous media
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The modification of natural phosphate (NP) with sodium nitrate by calcination produces an extremely efficient basic catalyst for the Claisen-Schmidt condensation. A large variety of chalcones is easily obtained in high yield at room temperature using only a catalytic amount of NaNO3/NP.
- Sebti, Sa?d,Solhy, Abderrahim,Tahir, Rachid,Boulaajaj, Sa?d,Mayoral, José A.,Fraile, José M.,Kossir, Abdelali,Oumimoun, Hammou
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p. 7953 - 7955
(2007/10/03)
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- Electronic effects in the regioselectivity of nucleophilic attacks on cationic 1,3-diaryl-π-allylpalladium complexes
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Nucleophilic attacks on π-allylpalladium complexes derived from O2N-Ph-(CH-CH-CH)-Ph-X systems (X = 4-OMe and 4-Cl) occur preferentially at the allylic terminus remote from the electron-withdrawing group (NO2).
- Prat,Ribas,Moreno-Manas
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p. 1695 - 1706
(2007/10/02)
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- Interactive free energy relationships for non-additive multiple substituent effects in base catalysed condensation of benzaldehydes with acetophenones: A kinetic study
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The base-catalysed condensation of benzaldehydes with acetophenones is enhanced by electron-withdrawing substituents in both starting compounds.The magnitude of ρ-value obtained for various substituents in the benzaldehyde moiety decreases with the introduction of electron-withdrawing groups in the para position of acetophenone moiety.
- Sondu, S.,Sethuram, B,Rao, T. Navaneeth
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- Co-condensation of 2-Aminopyridine, Aromatic Aldehydes, and Ketones
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The co-condensation of 2-aminopyridine with aromatic aldehydes and ketones proceeds via the initial formation from the amine and the benzaldehydes of (2-pyridylamino)aryl carbinols, which then react with p-nitroacetophenone to give 3-aryl-1-(4-nitrophenyl
- Letunov, V. I.,Soldatova, N. P.
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p. 861 - 864
(2007/10/02)
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- SYNTHESIS OF 1,3-DIARYL-4,7-PHENANTHROLINES
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A number of new 1,3-diaryl-4,7-phenanthrolines were synthesized by heterocyclization of arylidene-6-quinolylamines with acetophenones in the presence of an acidic catalyst.Intermediate amino ketones and side products, viz., N-(R1-benzyl)-6-quinolylamines and α,β-unsaturated ketones, were isolated.The IR, UV, PMR, and mass spectra of the synthesized compounds are discussed.
- Kozlov, N. S.,Gusak, K. N.,Serzhanina, V. A.,Krot, N. A.
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p. 1151 - 1154
(2007/10/02)
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- REACTION OF SCHIFF BASES OBTAINED FROM 4-AMINOANTIPYRINE AND 4-AMINO-1,2,4-TRIAZOLE WITH KETONES
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With acetophenone and p-nitroacetophenone in alcohol and benzene media in the presence of acid N-arylidene-4-aminoantipyrines form α,β-unsaturated ketones, and with antipyrine the form aryldiantipyrylmethanes.With the same ketones N-arylidene-4-amino-1,2,4-triazoles form the products from addition at the azomethine bond.In both cases reaction with benzylideneacetone was not detected.
- Letunov, V. I.
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p. 145 - 149
(2007/10/02)
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- REACTION OF 2-(ARYLIDENEAMINO)ETHANOLS WITH CARBONYL COMPOUNDS
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With acetophenone and p-nitroacetophenone in the presence of catalytic amounts of acid 2-(arylideneamino)ethanols form α,β-unsaturated ketones, and with antipyrine they form products from addition at the azomethine bond.
- Letunov, V. I.
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p. 2152 - 2154
(2007/10/02)
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- Synthesis and Biological Activity of Some New 10-phenothiazines
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Fourteen 10-phenothiazines (IV) have been synthesized via condensation of 10-hydrazino-acetylphenothiazine with substituted benzalacetophenones.These compounds inhibit 33-86percent in vitro activity of rat brain pyruvate oxidase and afford protection against pentylenetetrazol induced seizures in albino mice.However, their anticonvulsant properties are found to be independent of their pyruvate oxidase inhibitory activity.
- Jaiswal, Neelam,Jaiswal, R. K.,Barthwal, J. P.,Kishor, K.
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p. 252 - 253
(2007/10/02)
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