83909-69-7Relevant academic research and scientific papers
Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site
Meijer, Femke A.,Van Den Oetelaar, Maxime C. M.,Doveston, Richard G.,Sampers, Ella N. R.,Brunsveld, Luc
supporting information, p. 631 - 639 (2021/04/07)
The nuclear receptor RORγt is a key positive regulator in the differentiation and proliferation of T helper 17 (Th17) cells and the production of proinflammatory cytokines like IL-17a. Dysregulation of this pathway can result in the development of various
A highly efficient copper-catalyzed method for the synthesis of 2-hydroxybenzamides in water
Balkrishna, Shah Jaimin,Kumar, Sangit
, p. 1417 - 1426 (2012/06/30)
An efficient copper-catalyzed synthetic method for the preparation of 2-hydroxybenzamides is described for the first time from 2-chlorobenzamide substrates using copper iodide/1,10-phenanthroline and a base, potassium hydroxide, in neat water. By using this reaction, a series of 2-hydroxybenzamides with functional groups such as fluoro, chloro, iodo, methoxy, amide, and alcohol have been obtained in 33-96% yield. Other aromatic 2-chloroarylamides such as naphthalene, pyridine, and thiophene are found to be equally compatible to the reaction. It is proposed that the reaction proceed via formation of copper-amide complex, which may facilitate the hydroxylation in water. Overall, the first report on copper-catalyzed hydroxylation reaction in water and first catalytic route for the synthesis of 2-hydroxybenzamides is presented. Simple purification procedure and convenience of employing low-cost reagents in neat water make this method practical and economical for the synthesis of 2-hydroxybenzamides. Georg Thieme Verlag Stuttgart · New York.
Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis
Hwang, Jong Yeon,Smithson, David,Connelly, Michele,Maier, Julie,Zhu, Fangyi,Guy, Kiplin R.
supporting information; experimental part, p. 149 - 152 (2010/04/29)
A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.
