- Synthesis and Biological Screening of Novel 5-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole Derivatives
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A new series of 5-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole (6a-o) have been synthesized by a cyclocondensation reaction of ethyl 5-(4-chlorophenyl)-1-phenyl-1H-pyrazole-3-carboxylate (3a-c) with aryl imidoxime (5a-e). The newly synthesize
- Agrawal, Brijmohan R.,Farooqui, Mazahar,Khandebharad, Amol U.,Kulkarni, Pravin S.,Sarda, Swapnil R.
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p. 209 - 215
(2022/01/06)
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- La(OTf)3-catalysed one-pot synthesis of pyrazole tethered imidazo[1,2-: A] azine derivatives and evaluation of their light emitting properties
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A facile and efficient protocol has been unfolded towards the diversity-oriented synthesis of highly fluorescent pyrazole C-3(5) tethered imidazo[1,2-a]azines via an La(OTf)3 catalysed one-pot multicomponent assembly of pyrazole carbaldehydes, 2-aminoazines and isonitriles. This present protocol offers several advantages such as multiple bond formation in a single step, low catalyst loading, short reaction time, appreciable atom economy, good functional group tolerance, scalability and easy to perform reaction conditions. The optical properties of pyrazolyl imidazo[1,2-a]azines were also studied, and they exhibited an excellent fluorescence quantum yield (ΦF up to 83%).
- Sharma, Shubham,Paul, Avijit Kumar,Singh, Virender
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supporting information
p. 684 - 694
(2020/01/31)
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- Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors
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Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays an important role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol, which is implicated in many physiological processes. Beyond the possible utilization of MA
- Aghazadeh Tabrizi, Mojgan,Baraldi, Pier Giovanni,Baraldi, Stefania,Ruggiero, Emanuela,De Stefano, Lucia,Rizzolio, Flavio,Di Cesare Mannelli, Lorenzo,Ghelardini, Carla,Chicca, Andrea,Lapillo, Margherita,Gertsch, Jürg,Manera, Clementina,Macchia, Marco,Martinelli, Adriano,Granchi, Carlotta,Minutolo, Filippo,Tuccinardi, Tiziano
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p. 1340 - 1354
(2018/02/17)
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- Synthesis of new pyrazole-triazole hybrids by click reaction using a green solvent and evaluation of their antitubercular and antibacterial activity
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A new series of pyrazole-based 1,2,3-triazole derivatives (6a-x) were synthesized by employing click reaction using a 2:1 mixture of PEG-400 and water as green solvent. The synthesized intermediate and final compounds were characterized by 1H NMR, 13C NMR, and mass spectra and elemental analysis techniques. The structure of one of the final compounds, 6a was evidenced by single crystal X-ray diffraction study. Among the twenty-four compounds, five compounds (6a, 6b, 6d, 6f, and 6g) showed significant antitubercular activity against Mycobacterium tuberculosis H37Rv with a minimum inhibitory concentration (MIC) ≤ 6.25 μg/mL. The 4-(((5-(4-Chlorophenyl)-1-phenyl-1H-pyrazol-3-yl)methoxy)methyl)-1-cyclohexyl-1H-1,2,3-triazole (6g) was the most potent compound of the series, which showed a MIC of 3.13 μg/mL. The cytotoxicity study of active anti-TB compounds on normal Vero cells revealed that the compounds are non-toxic with a high selectivity index (>37). Most of the pyrazole-1,2,3-triazole derivatives with a 4-chlorophenyl substitution at position-5 of the pyrazole ring showed a better anti-TB activity than the corresponding 4-bromophenyl or 4-methoxyphenyl substituted derivatives. The target compounds were also evaluated for their in vitro antibacterial activity and six compounds (6a, 6c, 6d, 6e, 6l, and 6w) showed promising inhibition activity against four tested strains.
- Nayak, Nagabhushana,Ramprasad, Jurupula,Dalimba, Udayakumar,Yogeeswari, Perumal,Sriram, Dharmarajan,Kumar, H. S. Santosh,Peethambar,Achur, Rajeshwara
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p. 3721 - 3741
(2016/04/05)
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- Synthesis, anti-HSV-1, and cytotoxic activities of some new pyrazole- and isoxazole-based heterocycles
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Abstract Ethyl 2,4-dioxo-4-(p-chloro)phenylbutyrate 2 obtained by condensation of 4-chloroacetophenone with diethyl oxalate was converted to 5-(4-chlorophenyl)-1- phenyl-1H-pyrazole-3-carbohydrazide 5 and 5-(4-chlorophenyl) isoxazole-3-carbohydrazide 6 in
- Dawood, Kamal M.,Abdel-Gawad, Hassan,Mohamed, Hanan A.,Badria, Farid A.
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scheme or table
p. 912 - 919
(2012/05/07)
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- Structural study of diarylazoles related to Rimonabant
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The structures of three diarylazoles (two pyrazoles and one 1,2,4-triazole) related to Rimonabant have been determined by X-ray crystallography. The conformation of both aryl groups in the new structures is discussed with regard to other related compounds
- Alkorta, Ibon,Alvarado, Mario,Elguero, José,García-Granda, Santiago,Goya, Pilar,Torre-Fernández, Laura,Menéndez-Taboada, Laura
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experimental part
p. 82 - 89
(2009/06/27)
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- Antiobesity designed multiple ligands: Synthesis of pyrazole fatty acid amides and evaluation as hypophagic agents
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Searching for new antiobesity agents, a new series of fatty acid amide derivatives of 1,5-diarylpyrazole have been synthesized as dual peroxisome proliferator activated receptor alpha (PPARα)/cannabinoid receptor ligands. The compounds have been evaluated in vivo and in vitro as PPARα activators and as cannabinoids in two tests of the mouse tetrad. In vivo, food intake studies have been performed with all the compounds. No significant cannabinoid activity has been found but some compounds behaved as potent PPARα activators. Several compounds showed anorexigenic properties reducing food intake in rats.
- Alvarado, Mario,Goya, Pilar,Macias-Gonzalez, Manuel,Pavon, Francisco Javier,Serrano, Antonia,Jagerovic, Nadine,Elguero, Jose,Gutierrez-Rodriguez, Angel,Garcia-Granda, Santiago,Suardiaz, Margarita,Rodriguez de Fonseca, Fernando
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experimental part
p. 10098 - 10105
(2009/04/06)
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