24242-97-5Relevant articles and documents
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase
Even?s, Johan,Edfeldt, Fredrik,Lepist?, Matti,Svitacheva, Naila,Synnergren, Anna,Lundquist, Britta,Gr?nse, Mia,R?nnholm, Anna,Varga, Mikael,Wright, John,Wei, Min,Yue, Sherrie,Wang, Junfeng,Li, Chong,Li, Xuan,Chen, Gang,Liao, Yong,Lv, Gang,Tj?rnebo, Ann,Narjes, Frank
supporting information, p. 1315 - 1321 (2014/03/21)
The identification of novel, non-purine based inhibitors of xanthine oxidase is described. After a high-throughput screening campaign, an NMR based counterscreen was used to distinguish actives, which interact with XO in a reversible manner, from assay artefacts. This approach identified pyrimidone 1 as a reversible and competitive inhibitor with good lead-like properties. A hit to lead campaign gave compound 41, a nanomolar inhibitor of hXO with efficacy in the hyperuricemic rat model after oral dosing.
Catalytic Friedel-Crafts acylation of alkoxy benzenes by ferric hydrogensulfate
Salehi, Peyman,Khodaei, Mohammad Mahdi,Zolfigol, Mohammad Ali,Zeinoldini, Shahpour
, p. 1367 - 1373 (2007/10/03)
Friedel-Crafts acylation of alkoxy benzenes is achieved efficiently by reaction with aliphatic acid anhydrides in the presence of catalytic amounts of ferric hydrogensulfate, Fe(HSO4)3, in nitromethane. Alkyl benzenes and aryl halides, as well as aromatic anhydrides, remain intact under these conditions.
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
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Page column 42, (2010/01/30)
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Ar, B, R1, R2, R3a, R3b, R4, R5, R6and m are as defined herein.