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Nalilu Suchetha Kumari - One of the best experts on this subject based on the ideXlab platform.
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synthesis of some new 4 styryltetrazolo 1 5 a Quinoxaline and 1 substituted 4 styryl 1 2 4 triazolo 4 3 a Quinoxaline derivatives as potent anticonvulsants
European Journal of Medicinal Chemistry, 2009Co-Authors: Shivananda Wagle, Airody Vasudeva Adhikari, Nalilu Suchetha KumariAbstract:4-Methyltetrazolo[1,5-a]Quinoxaline (3) was prepared by the azide cyclocondensation of 2-chloro-3-methylQuinoxaline (2). The reaction of 3 with aromatic aldehydes furnished 4-styryltetrazolo[1,5-a]Quinoxalines (4a-f). Compound 2, on treatment with hydrazine hydrate gave 2-hydrazino-3-methylQuinoxaline (5). The ring closure of 5 was achieved by the reaction of orthoesters and trifluoroacetic acid to yield 4-methyl-1-(substituted)[1,2,4]triazolo[4,3-a]Quinoxalines (7a-c). Further, reaction of 7a-c with different aromatic aldehydes furnished the title compounds, 4-styryl-1-(substituted)[1,2,4]triazolo[4,3-a]Quinoxalines (8a-i) in good yield. In another scheme, the hydrazino compound 5 was treated with different aromatic aldehydes to yield corresponding N-arylidenehydrazino Quinoxalines (6a-d). Further, the oxidative cyclization of hydrazones by nitrobenzene yielded 1-aryl-4-methyl[1,2,4]triazolo[4,3-a]Quinoxalines (7d-g), which on condensation with aromatic aldehydes gave the title compounds, 1-aryl-4-styryl[1,2,4]triazolo[4,3-a]Quinoxalines (8j-u). The newly synthesized compounds have been characterized by FTIR, (1)H NMR, (13)C NMR and mass spectral data, followed by elemental analysis. Some of the compounds were screened for in vivo anticonvulsant activity. Few of them exhibited promising results.
Mahendra Nath - One of the best experts on this subject based on the ideXlab platform.
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an eco friendly pictet spengler approach to pyrrolo and indolo 1 2 a Quinoxalines using p dodecylbenzenesulfonic acid as an efficient broensted acid catalyst
ChemInform, 2015Co-Authors: Amreeta Preetam, Mahendra NathAbstract:An efficient, facile, and environmentally friendly method for the synthesis of various pyrrolo[1,2-a]Quinoxaline, dihydropyrrolo[1,2-a]Quinoxaline, and spiro[indoline-3,4′-pyrrolo[1,2-a]quinoxalin]-2-one derivatives under mild reaction conditions is developed.
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an eco friendly pictet spengler approach to pyrrolo and indolo 1 2 a Quinoxalines using p dodecylbenzenesulfonic acid as an efficient bronsted acid catalyst
RSC Advances, 2015Co-Authors: Amreeta Preetam, Mahendra NathAbstract:A facile and environmentally benign Pictet–Spengler strategy for the synthesis of a series of biologically important pyrrolo- and indolo[1,2-a]Quinoxalines has been developed by reacting 1-(2-aminophenyl)-pyrrole or 1-(2-aminophenyl)indoles with a wide range of aromatic aldehydes, acetophenones or isatins in ethanol at ambient temperature using p-dodecylbenzenesulfonic acid (p-DBSA) as an efficient Bronsted acid–surfactant combined catalyst. This methodology was found to be applicable to generate diverse Quinoxaline derivatives in fairly good yields under mild reaction conditions.
Zhenghong Zhou - One of the best experts on this subject based on the ideXlab platform.
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stereocontrolled construction of 4 5 dihydropyrrolo 1 2 a Quinoxaline scaffolds via chiral phosphoramidate catalyzed pictet spengler type reaction
Tetrahedron-asymmetry, 2016Co-Authors: Yuehua Wang, Youming Wang, Zhenghong ZhouAbstract:Abstract An efficient catalytic asymmetric synthesis of 4,5-dihydropyrrolo[1,2- a ]Quinoxalines has been developed on the basis of the Pictet–Spengler-type condensation of 1-(2-aminophenyl)pyrrole with a wide range of aldehydes. Structurally diverse 4,5-dihydropyrrolo[1,2- a ]Quinoxaline derivatives were obtained from 1-(2-aminophenyl)pyrrole and both aromatic and aliphatic aldehydes in good yields with moderate to good enantioselectivities upon treatment with chiral phosphoramidate catalyst IVb .
Jean Guillon - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of novel substituted pyrrolo 1 2 a Quinoxaline derivatives as inhibitors of the human protein kinase ck2
European Journal of Medicinal Chemistry, 2013Co-Authors: Jean Guillon, Marc Le Borgne, Charlotte Rimbault, Stephane Moreau, Solene Savrimoutou, Noel Pinaud, Sophie BaratinAbstract:Abstract Herein we describe the synthesis and properties of substituted phenylaminopyrrolo[1,2-a]Quinoxaline-carboxylic acid derivatives as a novel class of potent inhibitors of the human protein kinase CK2. A set of 15 compounds was designed and synthesized using convenient and straightforward synthesis protocols. The compounds were tested for inhibition of human protein kinase CK2, which is a potential drug target for many diseases including inflammatory disorders and cancer. New inhibitors with IC50 in the micro- and sub-micromolar range were identified. The most promising compound, the 4-[(3-chlorophenyl)amino]pyrrolo[1,2-a]Quinoxaline-3-carboxylic acid 1c inhibited human CK2 with an IC50 of 49 nM. Our findings indicate that pyrrolo[1,2-a]Quinoxalines are a promising starting scaffold for further development and optimization of human protein kinase CK2 inhibitors.
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synthesis antimalarial activity and molecular modeling of new pyrrolo 1 2 a Quinoxalines bispyrrolo 1 2 a Quinoxalines bispyrido 3 2 e pyrrolo 1 2 a pyrazines and bispyrrolo 1 2 a thieno 3 2 e pyrazines
Journal of Medicinal Chemistry, 2004Co-Authors: Jean Guillon, Philippe Grellier, Mehdi Labaied, Pascal Sonnet, Jeanmichel Leger, Rebecca Deprezpoulain, Isabelle Forfarbares, Patrick Dallemagne, Nicolas Lemaitre, Fabienne PehourcqAbstract:Three pyrrolo[1,2-a]Quinoxalines, 15 bispyrrolo[1,2-a]Quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines were synthesized from various substituted nitroanilines or nitropyridines and tested for their in vitro activity upon the erythrocytic development of Plasmodium falciparum strains with different chloroquine-resistance status. Bispyrrolo[1,2-a]Quinoxalines showed superior antimalarial activity with respect to monopyrrolo[1,2-a]Quinoxalines. The best activity was observed with bispyrrolo[1,2-a]Quinoxalines linked by a bis(3-aminopropyl)piperazine. Moreover, it was observed that the presence of a methoxy group on the pyrrolo[1,2-a]Quinoxaline nucleus increased the pharmacological activity. Drug effects upon β-hematin formation were assayed and showed similar or higher inhibitory activities than CQ. A possible mechanism of interaction implicating binding of pyrroloQuinoxalines to β-hematin was supported by molecular modeling.
Jesus Galvez - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of 4 alkoxy 6 9 dichloro 1 2 4 triazolo 4 3 a Quinoxalines as inhibitors of tnf α and il 6
European Journal of Medicinal Chemistry, 2012Co-Authors: Antonio Guirado, Jose Lopez I Sanchez, Antonio J Ruizalcaraz, Delia Bautista, Jesus GalvezAbstract:Abstract An efficient synthetic method for previously unattainable 4-alkoxy-6,9-dichloro[1,2,4]triazolo[4,3- a ]Quinoxalines has been established. Reactions between 5,8-dichloro-2,3-dicyanoQuinoxaline and alcohols in the presence of triethylamine led to 3-alkoxy-5,8-dichloro-2-cyanoQuinoxalines in high to quantitative yields. These compounds were treated with hydrazine giving 3-alkoxy-5,8-dichloro-2-hydrazinoQuinoxalines in near quantitative yields, that reacted with triethyl orthoformate to provide the title compounds in high yields. The molecular structure of a member of this family of compounds: 6,9-dichloro-4-ethoxy[1,2,4]triazolo[4,3- a ]Quinoxaline, was determined by X-ray crystallography. The series of compounds synthesized were evaluated for their potential anti-inflammatory activity as inhibitors of the pro-inflammatory cytokines TNF-α and IL-6. Compounds 8e , 8a , 8b and 8g presented simultaneously good levels of inhibition of both cytokines being compound 8e the most concomitantly potent one. Compounds 8d , 8f and 8h specifically inhibited IL-6 with no significant inhibition of TNF-α. Compound 8c was not significantly active upon TNF-α, and showed no activity upon IL-6.
