89873-42-7Relevant academic research and scientific papers
Agonists for the adenosine A1 receptor with tunable residence time. a case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines
Louvel, Julien,Guo, Dong,Agliardi, Marta,Mocking, Tamara A. M.,Kars, Roland,Pham, Tan Phát,Xia, Lizi,De Vries, Henk,Brussee, Johannes,Heitman, Laura H.,Ijzerman, Adriaan P.
, p. 3213 - 3222 (2014/05/20)
We report the synthesis and evaluation of previously unreported 4-amino-6-aryl-5-cyano-2-thiopyrimidines as selective human adenosine A 1 receptor (hA1AR) agonists with tunable binding kinetics, this without affecting their nanomolar affinity for the target receptor. They show a very diverse range of kinetic profiles (from 1 min (compound 52) to 1 h (compound 43)), and their structure-affinity relationships (SAR) and structure-kinetics relationships (SKR) were established. When put in perspective with the increasing importance of binding kinetics in drug discovery, these results bring new evidence of the consequences of affinity-only driven selection of drug candidates, that is, the potential elimination of slightly less active compounds that may display preferable binding kinetics.
5-Aryl-4-hydroxy-3(2H)-isothiazolone 1,1-Dioxide Derivatives. Synthesis and 13C NMR Characterization
Rooney, C. S.,Cochran, D. W.,Ziegler, C.,Cragoe, E. J.,Williams, H. W. R.
, p. 2212 - 2217 (2007/10/02)
5-Phenyl- and 5-thiazolyl-4-hydroxy-3(2H)-isothiazolone 1,1-dioxide derivatives have been prepared by base-catalyzed cyclocondensation of diethyl oxalate with an arylmethanesulfonamide, as well as by reaction of an arylmethanesulfonamide with methyl or et
4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis
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, (2008/06/13)
4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: STR1 where X and Y are independently selected from the group consisting of hydrogen, halogen, and C1-6 alkyl; provided that positions 2 and 6 of the substituted
