- Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines
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A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity a
- Marchand, Pascal,Bazin, Marc-Antoine,Pagniez, Fabrice,Rivière, Guillaume,Bodero, Lizeth,Marhadour, Sophie,Nourrisson, Marie-Renée,Picot, Carine,Ruchaud, Sandrine,Bach, Stéphane,Baratte, Blandine,Sauvain, Michel,Pareja, Denis Castillo,Vaisberg, Abraham J.,Le Pape, Patrice
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- One-pot synthesis of 6H-2,2a1,3-triazaaceanthrylen-6-ones and 6H-2,2a1,4-triazaaceanthrylen-6-ones via tandem cyclization strategies
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Two operationally simple one-pot protocols have been developed for the synthesis of 6H-2,2a1,3-triazaaceanthrylen-6-ones and 6H-2,2a1,4-triazaaceanthrylen-6-ones. The first Pd-catalyzed tandem cyclization of imidazo[1,2-a]pyrimidines/imidazo[1,2-a]pyrazines with 2-chlorobenzaldehydes could proceed in aqueous medium under air, affording the desired products in moderate to good yields. The molecular structures of products 3i and 5b were confirmed by X-ray crystallographic analysis.
- Mu, Bing,Li, Jingya,Zou, Dapeng,Wu, Yusheng,Chang, Junbiao,Wu, Yangjie
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supporting information
p. 4816 - 4821
(2017/12/07)
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- IMIDAZOPYRAZINES AND PYRAZOLOPYRIMIDINES AND THEIR USE AS AMPA RECEPTOR MODULATORS
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Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, [Formula should be inserted here] Also provided herein are pharmaceutical compositions, comprising compounds of Formula (I), and methods of
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Page/Page column 100
(2016/12/26)
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- General Method for the Preparation of Electron-Deficient Imidazo[1,2-a]pyridines and Related Heterocycles
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A new annulation method for the preparation of the imidazo[1,2-a]pyridine ring system under mild conditions is presented. Treatment of a 2-aminopyridine with a dimethylketal tosylate in acetonitrile at elevated temperature (80-140°C) in the presence of catalytic Sc(OTf)3 provides the imidazo[1,2-a]pyridine product in good yield. The annulation method is broadly applicable to electron-poor 2-aminopyridines and displays a complementary profile to the classic preparation of the imidazo[1,2-a]pyridine ring system by reaction of a bromoketone with electron-rich and -neutral substrates. The scope of the process and mechanistic considerations are discussed.
- McDonald, Ivar M.,Peese, Kevin M.
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p. 6002 - 6005
(2016/01/09)
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- Structure activity relationship studies of imidazo[1,2-a]pyrazine derivatives against cancer cell lines
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Designed novel imidazo[1,2-a]pyrazine based inhibitors, synthesized by condensing α-aminopyrazines with α-halocarbonyl compounds followed by electrophilic substitutions. Cytotoxic effects on four cancer cell lines evaluated. Based on preliminary data, imidazo[1,2-a]pyrazine template redesigned to improve activity.
- Myadaraboina, Shailaja,Alla, Manjula,Saddanapu, Venkateshwarlu,Bommena, Vittal Rao,Addlagatta, Anthony
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experimental part
p. 5208 - 5216
(2011/01/04)
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