53937-03-4Relevant academic research and scientific papers
HETEROCYCLIC WDR5 INHIBITORS AS ANTI-CANCER COMPOUNDS
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Page/Page column 100-101, (2021/02/19)
The present invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; (I) which are inhibitors of WDR5. The present invention also provides pharmaceutical compositions comprising such compounds, compositions comprising such compounds with an additional therapeutic agent and the therapeutic uses of such compounds.
Umpolung-like Cross-coupling of Tosylhydrazones with 4-Hydroxy-2-pyridones under Palladium Catalysis
Katsina, Tania,Papoulidou, Kyriaki Eleni,Zografos, Alexandros L.
supporting information, p. 8110 - 8115 (2019/10/11)
Tosylhydrazones under palladium catalysis were found to perform cross-coupling reactions with 4-hydroxy-2-pyridones. The umpolung-like reactivity, between the α-carbon of tosylhydrazone and the 3-position of the heterocycle, which is observed in the obtai
TRICYCLIC GYRASE INHIBITORS FOR USE AS ANTIBACTERIAL AGENTS
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Paragraph 0260; 0261, (2014/04/03)
Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: Intelligent design and evolution through the judicious use of structure-guided design and stucture-activity relationships
Charifson, Paul S.,Grillot, Anne-Laure,Grossman, Trudy H.,Parsons, Jonathan D.,Badia, Michael,Bellon, Steve,Deininger, David D.,Drumm, Joseph E.,Gross, Christian H.,LeTiran, Arnaud,Liao, Yusheng,Mani, Nagraj,Nicolau, David P.,Perola, Emanuele,Ronkin, Steven,Shannon, Dean,Swenson, Lora L.,Tang, Qing,Tessier, Pamela R.,Tian, Ski-Kai,Trudeau, Martin,Wang, Tiansheng,Wei, Yunyi,Zhang, Hong,Stamos, Dean
experimental part, p. 5243 - 5263 (2009/07/01)
The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV are well-characterized clinically validated targets of the fluoroquinolone antibiotics which exert their antibacterial activity through inhibition of the catalytic subunits. Inhibition of these targets through interaction with their ATP sites has been less clinically successful. The discovery and characterization of a new class of low molecular weight, synthetic inhibitors of gyrase and topoisomerase IV that bind to the ATP sites are presented. The benzimidazole ureas are dual targeting inhibitors of both enzymes and possess potent antibacterial activity against a wide spectrum of relevant pathogens responsible for hospital- and community-acquired infections. The discovery and optimization of this novel class of antibacterials by the use of structure-guided design, modeling, and structure-activity relationships are described. Data are presented for enzyme inhibition, antibacterial activity, and in vivo efficacy by oral and intravenous administration in two rodent infection models.
A practical procedure for the selective N-alkylation of 4-alkoxy-2-pyridones and its use in a sulfone-mediated synthesis of N-methyl-4-methoxy-2-pyridone
Conreaux, David,Bossharth, Emmanuel,Monteiro, Nuno,Desbordes, Philippe,Balme, Geneviève
, p. 7917 - 7920 (2007/10/03)
It has been found that selective N-alkylation of 4-alkoxy-2-pyridones can be achieved under anhydrous, mild conditions with tetrabutylammonium iodide and potassium tert-butoxide being employed as the catalyst and the base, respectively. The procedure was applied to the preparation of 4-methoxy-1-methyl-2-pyridone, a valuable building block for heterocycle synthesis.
SUBSTITUTED PYRIDINONES
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Page/Page column 251-252, (2008/06/13)
Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Novel sulfonate analogues of combretastatin A-4: Potent antimitotic agents
Gwaltney II, Stephen L.,Imade, Hovis M.,Barr, Kenneth J.,Li, Qun,Gehrke, Laura,Credo,Warner, Robert B.,Lee, Jang Yun,Kovar, Peter,Wang, Jieyi,Nukkala, Michael A.,Zielinski, Nicolette A.,Frost, David,Ng, Shi-Chung,Sham, Hing L.
, p. 871 - 874 (2007/10/03)
Sulfonate analogues of combretastatin A-4 have been prepared. These compounds compete with colchicine and combretastatin A-4 for the colchicine binding site on tubulin and are potent inhibitors of tubulin polymerization and cell proliferation. Importantly, these compounds also inhibit the proliferation of P-glycoprotein positive (+) cancer cells, which are resistant to many other antitumor agents.
Cycloadditions in Syntheses. Part 28. 2-Azabicyclohexane-3,5-dione and its Derivatives: Synthesis and Transformation to Azetidin-2-ones
Katagiri, Nobuya,Sato, Masayuki,Yoneda, Naoki,Saikawa, Satoshi,Sakamoto, Toshiyuki,et al.
, p. 1289 - 1296 (2007/10/02)
2-Azabicyclohexane-3,5-dione has been synthesized via photopyridone formation from 4-(dimethyl-t-butylsiloxy)- or 4-alkoxy-2-pyridones followed by mild acid hydrolysis.The title compound and its derivatives react with a variety of nucleophiles (ROH
