91713-56-3Relevant academic research and scientific papers
Efficient Friedel–Crafts benzoylation of aniline derivatives with 4-fluorobenzoyl chloride using copper triflate in the synthesis of aminobenzophenones
Tran, Phuong Hoang,Phung, Huy Quang,Hansen, Poul Erik,Tran, Hai Ngoc,Le, Thach Ngoc
, p. 893 - 901 (2016/07/06)
ABSTRACT: An efficient pathway for the synthesis of the aminobenzophenone derivatives via Friedel–Crafts benzoylation using copper triflate as catalyst is proposed. New derivatives are synthesized. The copper triflate could be easily recovered and reused without loss of catalytic activity. Both the use of ionic liquids and microwave heating turned out to be fruitful.
2,3-Diaryl-substituted indole based COX-2 inhibitors as leads for imaging tracer development
Laube, Markus,Tondera, Christoph,Sharma, Sai Kiran,Bechmann, Nicole,Pietzsch, Franz-Jacob,Pigorsch, Arne,Koeckerling, Martin,Wuest, Frank,Pietzsch, Jens,Kniess, Torsten
, p. 38726 - 38742 (2014/11/08)
A series of 2,3-diaryl-substituted indoles containing a fluorine or methoxy group was synthesized via Fischer indole synthesis, McMurry cyclization, or Bischler-Moehlau reaction to identify potential leads for positron emission tomography (PET) radiotracer development as well as for optical imaging. All 2,3-diaryl-substituted indoles possess autofluorescent properties with an emission maximum in a range of 443-492 nm, which is acceptable for biological studies in vitro and, in part, in vivo. The molecular structure of compounds 3a and 3j was confirmed by X-ray crystal structure analysis. COX inhibitory activity was evaluated by a fluorescence-based and enzyme immunoassay-based assay. Redox activity of all target compounds was also determined. All synthesized 2,3-diaryl-substituted indoles are inhibitors of COX-2 enzyme in the low micromolar range. Compounds 3e, 3f, 3g and 3m displayed a 30-40% inhibition of COX-2 at 0.1 μM concentration while compounds 3f and 3g also exhibited COX-1 inhibitory activity. Various compounds like 3g showed substantial antioxidative potential (RDIENE = 2.85, RHAVA = 1.98), an effect that was most measurable with methoxy-substituted compounds. With respect to PET radiotracer synthesis, OMe-containing compound 3j was selected as a promising candidate for carbon-11 labeling, and F-containing compound 3m as a lead for the development of a fluorine-18 labeled derivative. the Partner Organisations 2014.
Design and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase
Trejo, Alejandra,Arzeno, Humberto,Browner, Michelle,Chanda, Sushmita,Cheng, Soan,Comer, Daniel D.,Dalrymple, Stacie A.,Dunten, Pete,Lafargue, JoAnn,Lovejoy, Brett,Freire-Moar, Jose,Lim, Julie,McIntosh, Joel,Miller, Jennifer,Papp, Eva,Reuter, Deborah,Roberts, Rick,Sanpablo, Florentino,Saunders, John,Song, Kyung,Villasenor, Armando,Warren, Stephen D.,Welch, Mary,Weller, Paul,Whiteley, Phyllis E.,Zeng, Lu,Goldstein, David M.
, p. 4702 - 4713 (2007/10/03)
Inhibition of the biosynthesis of proinflammatory cytokines such as tumor necrosis factor and interleukin-1 via p38 has been an approach toward the development of a disease modifying agent for the treatment of chronic inflammation and autoimmune diseases.
