- Synthesis of some new n-acetylated pyrazoline derivatives via the efficient one-pot reaction by using p-toluenesulfonic acid
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A series of a new class of N-acetylated pyrazoline derivatives were synthesized by treatment of chalcones with hydrazine hydrate and acetic anhydride or oxalic acid in the presence of the catalytic amount of p-toluenesulfonic acid in ethanol. All synthesized products were characterized by FT-IR, 1H, and 13C NMR spectral data and elemental analyses. Some advantages of this protocol are a simple work-up procedure, time-consuming reaction and good to high yields.
- Khodadad, Hadis,Pourshamsian, Khalil,Hatamjafari, Farhad,Sadeghi, Babak
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p. 165 - 171
(2021/02/05)
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- Amine-functionalized nano-NaY zeolite for the synthesis of N-acetyl pyrazoles and dihydropyrimidines
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An efficient base-catalyzed synthesis of dihydropyrimidines and N-acetyl pyrazoles is reported using 1-(2-aminoethyl)piperazine-modified nano-NaY zeolite (ZeSi–AP) under mild and green conditions. The structure of the catalyst was identified by using FT-IR, XRD, TGA, DTA, DLS, SEM, TEM, and elemental analyses. This heterogeneous catalyst has many benefits, such as a simple work-up procedure, high product yield, and it is easily regenerated and reused at least for four cycles without losing its activity.
- Razavian Mofrad, Raheleh,Kabirifard, Hassan,Tajbakhsh, Mahmood,Firouzzadeh Pasha, Ghasem
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- Synthesis of some new n-acetylated pyrazoline derivatives via the efficient one-pot reaction by using p-toluenesulfonic acid
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A series of a new class of N-acetylated pyrazoline derivatives were synthesized by treatment of chalcones with hydrazine hydrate and acetic anhydride or oxalic acid in the presence of the catalytic amount of p-toluenesulfonic acid in ethanol. All synthesized products were characterized by FT-IR, 1H, and 13C NMR spectral data and elemental analyses. Some advantages of this protocol are a simple work-up procedure, timeconsuming reaction and good to high yields.
- Hatamjafari, Farhad,Khodadad, Hadis,Pourshamsian, Khalil,Sadeghi, Babak
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p. 165 - 171
(2020/10/06)
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- SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H
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Cathepsins have emerged as potential drug targets for melanoma therapy and engrossed attention of researchers for development and evaluation of cysteine cathepsin inhibitors as cancer therapeutics. In this direction, we have designed, synthesized, and ass
- Raghav, Neera,Singh, Mamta
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supporting information
p. 4233 - 4245
(2014/08/18)
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- Solvent-free synthesis of some1-acetyl pyrazoles
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Some N-acetyl pyrazoles including 1-(3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl) ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones like substituted styryl 3,4-dichlorophenyl
- Thirunarayanan, Ganesamoorthy,Sekar, Krishnamoorthy Guna
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p. 599 - 605
(2013/11/06)
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- Effect of ring A and ring B substitution on the cytotoxic potential of pyrazole tethered chalcones
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Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are collectively known as chalcones. The cytotoxic potential of chalcones which consists of C6-C 3-C6 units gets enhanced by the incorporation of pyrazole ring as proved by our earlier studies. Thus in the present work, pyrazoles of chalcones with ring A substituted by furan, naphthalene and variety of substituted phenyl rings has been prepared and evaluated for in vitro cytotoxic activity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines. Springer Science+Business Media, LLC 2011.
- Nepali, Kunal,Kadian, Kanika,Ojha, Ritu,Dhiman, Rajni,Garg, Atul,Singh, Gagandip,Buddhiraja, Abhishek,Bedi, Preet Mohinder Singh,Dhar, Kanaya Lal
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p. 2990 - 2997
(2012/10/29)
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- Anticonvulsant activity of a combined pharmacophore of pyrazolo-pyridines with lesser toxicity in mice
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Various 2-amino-6-[3-(substituted phenyl)-5-phenyl-4,5-dihydropyrazol-1-yl] -4-(substituted phenyl)nicotinonitriles (3a-t) were designed and synthesized by clubbing two active anticonvulsant pharmacophores pyrazole and pyridine. All the synthesized compounds possessed the pharmacophoric elements essential for good anticonvulsant activity. The anticonvulsant screening was performed by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) tests. Two compounds 3i and 3s showed significant anticonvulsant activity in both the screens with ED50 values 17.5 mg/kg and 22.6 mg/kg respectively in MES screen and 154.1 mg/kg and 242.6 mg/kg respectively in scPTZ screen. They were also found to have no acute toxic effects in mice when tested at elevated doses.
- Siddiqui, Nadeem,Ahsan, Waquar,Alam, M. Shamsher,Ali, Ruhi,Srivastava, Kamna,Ahmed, Sharique
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p. 576 - 582
(2011/12/03)
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- Enantioselective phase-transfer catalysis: Synthesis of pyrazolines
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All paired up: Under catalytic phase-transfer conditions the formation of a chiral ion pair between quininium cation 1 and hydrazine anion 2 led to an enantioselective aza-Michael cyclocondensation domino reaction to furnish pyrazolines. A convenient one-pot protocol allowed exchange of the functional group (R1) on the nitrogen atom.
- Make, Olivier,Dez, Isabelle,Levacher, Vincent,Briere, Jean-Francois
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supporting information; experimental part
p. 7072 - 7075
(2010/11/05)
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- TBD-organocatalysed synthesis of pyrazolines
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It was found that TBD, a cheap and commercially available guanidine, easily catalysed the synthesis of biologically important 3,5-diarylpyrazolines from chalcones and acylhydrazines via a selective secondary amine alkylation.
- Mahe, Olivier,Frath, Denis,Dez, Isabelle,Marsais, Francis,Levacher, Vincent,Briere, Jean-Franois
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supporting information; experimental part
p. 3648 - 3651
(2009/10/23)
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- A divergent approach to the synthesis of 3-substituted-2-pyrazolines: Suzuki cross-coupling of 3-sulfonyloxy-2-pyrazolines
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(Chemical Equation Presented) The efficient Suzuki cross-coupling of pyrazoline nonaflates with organoboron reagents was achieved to afford diverse 3-substituted-2-pyrazolines in excellent yield. The nonaflates displayed improved reactivity over the corre
- Grimm, Jonathan B.,Wilson, Kevin J.,Witter, David J.
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supporting information; experimental part
p. 6390 - 6393
(2009/12/06)
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- Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein
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A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein- mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.
- Manna, Fedele,Chimenti, Franco,Fioravanti, Rossella,Bolasco, Adriana,Secci, Daniela,Chimenti, Paola,Ferlini, Cristiano,Scambia, Giovanni
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p. 4632 - 4635
(2007/10/03)
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- Microwave assisted synthesis of 2-pyrazolines
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A simple and efficient method has been developed for the rapid synthesis of 1-acetyl-3, 5-diaryl-2-pyrazolines 2 from chalcones 1 and hydrazine hydrate in unmodified domestic microwave oven in unsealed borosil vessels using acetic acid as energy transfer medium. Rate enhancement with improved yield, a characteristic of the synthesis under microwave irradiation has been observed in the present paper. The compounds synthesised have been characterised and compared with samples prepared by thermal methods.
- Paul, Satya
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p. 1279 - 1282
(2007/10/03)
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- Heterocycles. 3. Synthesis and Spectral Data of Some 2-Pyrazolines
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The reaction of 1,3-diaryl-2-propen-1-ones (Ia-o) with hydrazine and methyl- and phenylhydrazine produced different substituted 2-pyrazolines (III).The structures of these products were evident from their chemical and spectroscopic analysis.
- El-Rayyes, Nizar R.,Hovakeemian, George H.,Hmoud, Hayat S.
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p. 225 - 229
(2007/10/02)
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