97760-94-6Relevant articles and documents
Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: Structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents
Suh, Young-Ger,Lee, Yong-Sil,Min, Kyung-Hoon,Park, Ok-Hui,Kim, Jin-Kwan,Seung, Ho-Sun,Seo, Seung-Yong,Lee, Bo-Young,Nam, Yeon-Hee,Lee, Kwang-Ok,Kim, Hee-Doo,Park, Hyeung-Geun,Lee, Jeewoo,Oh, Uhtaek,Lim, Ju-Ok,Kang, Sang-Uk,Kil, Min-Jung,Koo, Jae-Yeon,Shin, Song Seok,Joo, Yung-Hyup,Kim, Jin Kwan,Jeong, Yeon-Su,Kim, Sun-Young,Park, Young-Ho
, p. 5823 - 5836 (2007/10/03)
Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure-activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM.
Copper-catalyzed halogen exchange in aryl halides: An aromatic finkelstein reaction
Klapars, Artis,Buchwald, Stephen L.
, p. 14844 - 14845 (2007/10/03)
A mild and general method for the conversion of aryl, heteroaryl, and vinyl bromides into the corresponding iodides was developed utilizing a catalyst system comprising 5 mol % of Cul and 10 mol % of a 1,2- or 1,3-diamine ligand. A variety of polar functional groups are tolerated, and even N-H containing substrates such as sulfonamides, amides, and indoles are compatible with the reaction conditions. Both the reaction rate and the equilibrium conversion of the aryl bromide depend on the choice of the halide salt and the solvent. The best results were obtained using Nal as the halide salt and dioxane, n-butanol, or n-pentanol as the solvents. Copyright
Tetrazolyl-phenyl acetamide glucokinase activators
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, (2008/06/13)
Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.