- PIPERAZINE DERIVATIVES AS ANTIVIRAL AGENTS WITH INCREASED THERAPEUTIC ACTIVITY
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The present invention provides 2-phenylpiperazine derivatives having a benzofuran-2-yl group which contributes to increase the antiviral activity as well as, for some substituents, the CC50, giving more active and less cytotoxic compounds. Alth
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Page/Page column 21; 22
(2017/09/15)
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- New 4-Acyl-1-phenylaminocarbonyl-2-phenylpiperazine Derivatives as Potential Inhibitors of Adenovirus Infection. Synthesis, Biological Evaluation, and Structure-activity Relationships
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The search for human adenovirus (HAdV)-specific antiviral drugs for the treatment of HAdV infections in immunocompromised patients continues to be a challenging goal for medicinal chemistry. Here, we report the synthesis, biological evaluation, and struct
- Sánchez-Céspedes, Javier,Martínez-Aguado, Pablo,Vega-Holm, Margarita,Serna-Gallego, Ana,Candela, José Ignacio,Marrugal-Lorenzo, José Antonio,Pachón, Jerónimo,Iglesias-Guerra, Fernando,Vega-Pérez, José Manuel
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p. 5432 - 5448
(2016/07/06)
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- Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity
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Several 4-substituted 1-acylpiperazines, obtained by molecular simplification of 4-substituted 1,4-diazabicyclo[4.3.0]nonan-9-ones, have been synthesized and tested in vivo on the mouse passive avoidance test, to evaluate their nootropic activity. The results show that, apparently, an N-acylpiperazine group can mimic the 2-pyrrolidinone ring of 1,4-diazabicyclo[4.3.0]nonan-9-one, as the compounds of the new series maintain high nootropic activity. Moreover molecular simplification produces more clear-cut structure-activity relationships with respect to the parent series. The mechanism of action also appears to be similar in the two series. In fact, although the molecular mechanism remains to be elucidated, the most potent compound of each class (DM232 and 13, DM235) is able to increase acetylcholine release in rat brain. Piperazine derivatives represent a new class of nootropic drugs with an in vivo pharmacological profile very similar to that of piracetam, showing much higher potency with respect to the reference compound. Among the compounds studied, 13 (DM235) shows outstanding potency, being active at a dose of 0.001 mg kg-1 sc.
- Manetti,Ghelardini,Bartolini,Dei,Galeotti,Gualtieri,Romanelli,Teodori
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p. 4499 - 4507
(2007/10/03)
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- Studies on development of sufficiently chemoselective N-acylation reagents: N-Acyl-N-(2,3,4,5,6-pentafluorophenyl)methanesulfonamides
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A variety of storable N-acyl-N-(2,3,4,5,6-pentafluorophenyl)methanesulfonamides (4a-e) prepared from N-2,3,4,5,6-pentafluorophenylmethanesulfonamide (3), have been developed after systematic research on the structure-reactivity relationship and were found to serve as N-acylation reagents exhibiting sufficiently good chemoselectivity. (C) 2000 Elsevier Science Ltd.
- Kondo, Kazuhiro,Sekimoto, Erika,Nakao, Junko,Murakami, Yasuoki
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p. 5843 - 5856
(2007/10/03)
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- 2-chloro-N,N-dibenzoylaniline: A selective N-benzoylating reagent
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Highly selective benzoylation of a less hindered amino group in the presence of a more hindered amino group with 2-chloro-N,N-dibenzoylaniline (2d), a convenient to use and stable reagent, is described.
- Kondo, Kazuhiro,Murakami, Yasuoki
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p. 1217 - 1219
(2007/10/03)
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- A versatile synthon for chemoselective N-acylation reagents, 2-fluoro-N-mesylaniline
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2-Fluoro-N-mesylaniline 3b undergoes various N-acylalions easily to give 2-fluoro-N-acyl-N-mesylanilines 4b-8b, which function as good chemoselective N-acylation reagents, especially for benzyloxycarbonylation.
- Kondo, Kazuhiro,Sekimoto, Erika,Miki, Kazuki,Murakami, Yasuoki
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p. 2973 - 2974
(2007/10/03)
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- The Absolute Configurations of (+)- and (-)-2-Methylpiperazines and their N-Methyl Derivatives.
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S(-)-2-Methylpiperazinium dichloride was prepared by reduction of S(-)-3-methyl-2,5-dioxopiperazine (from glycyl-S-alanine) which established its absolute configuration.This dichloride and its enantiomer, R(+)-2-methylpiperazinium dichloride, were obtained in less optically pure forms by recrystallization of the diastereomeric RS-2-methylpiperazinium 2R,3R-di-O-benzoyltartrate salts followed by decomposition with a base.They were converted into S(+)- and R(-)-1,2,4-trimethylpiperazinium dichloride, S(+)- and R(-)-1,2,4,4-tetramethylpiperazinium iodide and S(+)- and R(-)-1,1,2,4,4-pentamethylpiperazinium diiodide.
- Armarego, Wilfred L. F.,Schou, Henning,Waring, Paul
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p. 1951 - 1966
(2007/10/02)
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