53222-92-7Relevant academic research and scientific papers
Highly efficient catalysts for the hydrogenation of nitro-substituted aromatics
Raja, Robert,Golovko, Vladimir B.,Thomas, John M.,Berenguer-Murcia, Angel,Zhou, Wuzong,Xie, Songhai,Johnson, Brian F. G.
, p. 2026 - 2028 (2005)
Nanoparticles of Co and NiPd, derived from colloidal precursors and supported on commercially available non-ordered mesoporous silica, are highly effective, cheap, recyclable and industrially viable catalysts for the hydrogenation of a range of nitro-substituted aromatics under mild conditions. The Royal Society of Chemistry 2005.
Pd-Pt/modified GO as an efficient and selective heterogeneous catalyst for the reduction of nitroaromatic compounds to amino aromatic compounds by the hydrogen source
Salahshournia, Hossein,Ghiaci, Mehran
, (2019/02/14)
In this work, different nitroaromatic compounds were successfully reduced to their corresponding aromatic amines with excellent conversion and selectivity in methanol at 50?°C by using Pd-Pt nanoparticles immobilized on the modified grapheme oxide (m-GO) and hydrogen as the reducing source. The catalytic efficiency of Pd and Pd-Pt loading on the modified GO was investigated for the reduction of various nitroaromatic compounds, and the Pd-Pt/m-GO system demonstrated the highest conversion and selectivity. The catalyst was characterized by different techniques including FT-IR, Raman, UV–Vis, XRD, BET, XPS, FESEM, EDS, and TEM. The metal nanoparticles with the size of less than 10?nm were uniformly distributed on the m-GO. The catalyst could be reused at least five times without losing activity, showing the stability of the catalyst structure. Finally, the efficiency of the prepared catalyst was compared with Pd-Pt/AC, and Pd-Pt/GO catalysts.
New potent biaryl sulfate-based hepatitis C virus inhibitors
You, Youngsu,Kim, Hee Sun,Bae, Il Hak,Lee, Seung Gi,Jee, Min Hyeok,Keum, Gyochang,Jang, Sung Key,Kim, B. Moon
, p. 87 - 100 (2016/09/23)
The discovery of a new series of potent hepatitis C virus (HCV) NS5A inhibitors containing biaryl sulfone or sulfate cores is reported. Structure-activity relationship (SAR) studies on inhibitors containing various substitution patterns of the sulfate or sulfone core structure established that m-,m′- substituted biaryl sulfate core-based inhibitors containing an amide moiety (compound 20) or an imidazole moiety (compound 24) showed extremely high potency. Compound 20 demonstrated double-digit pM potencies against both genotype 1b (GT-1b) and 2a (GT-2a). Compound 24 also exhibited double-digit pM potencies against GT-1b and sub nM potencies against GT-2a. Furthermore, compounds 20 and 24 exhibited no cardiotoxicity in an hERG ligand binding assay and showed acceptable plasma stability and no mutagenic potential in the Ames test. In addition, these compounds showed distinctive additive effects in combination treatment with the NS5B targeting drug sofosbuvir (Sovaldi). The results of this study showed that the compounds 20 and 24 could be effective HCV inhibitors.
Diphenyl sulfate derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating hepatitis C virus related diseases
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Paragraph 0182-0184, (2017/05/23)
The present invention relates to a diphenyl sulfate derivative or a pharmaceutically acceptable salt thereof, a production method thereof, and a pharmaceutical composition for preventing or treating hepatitis C virus-associated diseases containing the same as an active ingredient. According to the present invention, the diphenyl sulfate derivative excellently inhibits infection by hepatitis C virus and replication of hepatitis C virus, and thus can be useful as pharmaceutical compositions for preventing or treating liver diseases such as hepatocellular cancer, cirrhosis, chronic hepatitis C, and acute hepatitis C caused by hepatitis C virus.COPYRIGHT KIPO 2017
Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors
Kusuma, Bhaskar Reddy,Duerfeldt, Adam S.,Blagg, Brian S.J.
scheme or table, p. 7170 - 7174 (2012/01/15)
Novobiocin analogs lacking labile glycosidic ether have been designed, synthesized and evaluated for Hsp90 inhibitory activity. Replacement of the synthetically complex noviose sugar with simple aromatic side chains produced analogs that maintain moderate cytotoxic activity against MCF7 and SkBR3 breast cancer cell-lines. Rationale for the preparation of des-noviose novobiocin analogs in addition to their synthesis and biological evaluation are presented herein.
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring
Nourry, Arnaud,Zambon, Alfonso,Davies, Lawrence,Niculescu-Duvaz, Ion,Dijkstra, Harmen P.,Ménard, Delphine,Gaulon, Catherine,Niculescu-Duvaz, Dan,Suijkerbuijk, Bart M. J. M.,Manne, Frank Friedlos Helen A.,Kirk, Ruth,Whittaker, Steven,Marais, Richard,Springer, Caroline J.
supporting information; experimental part, p. 1964 - 1978 (2010/08/05)
We recently reported on the development of a novel series of BRAF inhibitors based on a tripartite A-B-C system characterized by a para-substituted central aromatic core connected to an imidazo[4,5]pyridin-2-one scaffold and a substituted urea linker. Here, we present a new series of BRAF inhibitors in which the central phenyl ring connects to the hinge binder and substrate pocket of BRAF with a meta-substitution pattern. The optimization of this new scaffold led to the development of lownanomolar inhibitors that permits the use of a wider range of linkers and terminal C rings while enhancing the selectivity for the BRAF enzyme in comparison to the para series.
2-IMIDAZOLINE, 2-OXAZOLINE, 2-THIAZOLINE, AND 4-IMIDAZOLE DERIVATIVES OF METHYLPHENYL, METHOXYPHENYL, AND AMINOPHENYL ALKYLSULFONAMIDES AND UREAS AND THEIR USE
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, (2008/06/13)
The present invention concerns novel compounds represented by the Formula: STR1 wherein: A is R 1 q (R 3 R 60 N). sub.m (Z)(NR 2) n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C=O or SO 2 ; n is 1 with the proviso that, when Z is C=O, m is 1; X is--NH--,--CH 2--, or--OCH 2--; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R 1 is H, lower alkyl, or phenyl, with the proviso that, when R 1 is H, m is 1; R 2, R 3, R 60 are each independently H, lower alkyl, or phenyl; R 4, R 5, R. sup.6, and R 7 are each independently hydrogen, lower alkyl,--CF. sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R. sup.2 and R 7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5-or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or--CN, with the proviso that, when R 7 is hydroxyl or lower alkylsulfonamido, then X is not--NH--when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R 1 SO 2 NR 2--), (R. sup.3 R 60 NSO 2 NR 2--), or (R 3 R 60 NCONR 2--). The invention also includes the use of the above compounds, and compositions containing them, as alpha 1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.
Phenyl-and aminophenyl-alkylsulfonamide and urea derivatives, their preparation and their use as alpha1A/1L adrenoceptor agonists
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, (2008/06/13)
The present invention concerns novel compounds represented by the Formula:*(formula 02)* wherein: A is R1q(R3R60N)m(Z)(NR2)n; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C=O or SO 2; n is 1 with the proviso that, when Z is C=O, m is 1; X is -NH-, -CH2-, or -OCH2-; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R 1 is H, lower alkyl, or phenyl, with the proviso that, when R1 is H, m is 1; R2, R3, R60 are each independently H, lower alkyl, or phenyl; R4, R5, R6, and R7 are each independently hydrogen, lower alkyl, - CF 3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R2 and R7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5-or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or -CN,with the proviso that, when R7 is hydroxyl or lower alkylsulfonamido, then X is not -NH- when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R1SO2NR2-), (R3R60NSO2NR2-), or (R3R60NCONR2-). The invention also includes the use of the above compounds, and compositions containing them, as alpha 1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.
Hydroxylation directe d'anilines en aminophenols
Jacquesy, Jean-Claude,Jouannetaud, Marie-Paule,Morellet, Guy,Vidal, Yves
, p. 625 - 629 (2007/10/02)
Anilines react with hydrogen peroxide in SbF5-HF to give aminophenols.The formation of the products can be accounted for by the reaction of the electrophile H3O2+ on the anilinium ions.For compounds 1a-4a, the reaction yields three possible aminophenols, the meta isomer being the major product.The process is more selective with ortho toluidine 5a and para toluidine 6a, giving aminophenol(s) 5c (42percent)) and 5e (21percent), and 6c (71percent), respectively.With meta toluidine 7a, only aminophenol 7d (35percent) can be isolated from the complex reaction mixture, ring substitution pattern of the substrate favoring para hydroxylation.
