124414-06-8Relevant academic research and scientific papers
Urea-Catalyzed Vinyl Carbocation Formation Enables Mild Functionalization of Unactivated C-H Bonds
Bagdasarian, Alex L.,Popov, Stasik,Wigman, Benjamin,Wei, Wenjing,Lee, Woojin,Nelson, Hosea M.
supporting information, p. 7775 - 7779 (2020/07/15)
Herein we report the 3,5-bistrifluoromethylphenyl urea-catalyzed functionalization of unactivated C-H bonds. In this system, the urea catalyst mediates the formation of high-energy vinyl carbocations that undergo facile C-H insertion and Friedel-Crafts re
Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers
Hofmann, Emily,Webster, Jonathan,Do, Thuy,Kline, Reid,Snider, Lindsey,Hauser, Quintin,Higginbottom, Grace,Campbell, Austin,Ma, Lili,Paula, Stefan
, p. 578 - 587 (2016/02/09)
In this study, we evaluated the abilities of a series of chalcones to inhibit the activity of the enzyme xanthine oxidase (XO) and to scavenge radicals. 20 mono- and polyhydroxylated chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and then tested for inhibitory potency against XO, a known generator of reactive oxygen species (ROS). In parallel, the ability of the synthesized chalcones to scavenge a stable radical was determined. Structure-activity relationship analysis in conjunction with molecular docking indicated that the most active XO inhibitors carried a minimum of three hydroxyl groups. Moreover, the most effective radical scavengers had two neighboring hydroxyl groups on at least one of the two phenyl rings. Since it has been proposed previously that XO inhibition and radical scavenging could be useful properties for reduction of ROS-levels in tissue, we determined the chalcones' effects to rescue neurons subjected to ROS-induced stress created by the addition of β-amyloid peptide. Best protection was provided by chalcones that combined good inhibitory potency with high radical scavenging ability in a single molecule, an observation that points to a potential therapeutic value of this compound class.
Syntheses of novel myxopyronin B analogs as potential inhibitors of bacterial RNA polymerase
Lira, Ricardo,Xiang, Alan X.,Doundoulakis, Thomas,Biller, William T.,Agrios, Konstantinos A.,Simonsen, Klaus B.,Webber, Stephen E.,Sisson, Wes,Aust, Robert M.,Shah, Amit M.,Showalter, Richard E.,Banh, Virginia N.,Steffy, Kevin R.,Appleman, James R.
, p. 6797 - 6800 (2008/09/16)
Based upon observations from our initial findings, additional myxopyronin B analogs have been prepared and tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against Escherichia coli and Staphylococcus
ANTITHROMBOTIC AROMATIC ETHERS
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Page/Page column 131-132, (2008/06/13)
This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.
Simple and Chemoselective Deprotection of Acetals Using Aqueous Dimethyl Sulfoxide
Kametani, Tetsuji,Kondoh, Hirotsune,Honda, Toshio,Ishizone, Hiroyuki,Suzuki, Yukio,Mori, Wakako
, p. 901 - 904 (2007/10/02)
Deprotection of acetals was achieved in aqueous dimethyl sulfoxide under neutral reaction condition.Selective cleavage of acyclic acetals bearing various types of acid labile protecting groups was also reported.
