106791-94-0Relevant academic research and scientific papers
Synthesis of 6-arylisocytosines and their potential for hydrogen bonding interactions
Patel, Alpa,Lewis, William,Searle, Mark S.,Stevens, Malcolm F.G.,Moody, Christopher J.
, p. 7339 - 7343 (2015/08/24)
Abstract The synthesis of a number of 6-arylisocytosines, including linked bis-isocytosines, from the reaction of guanidine with β-ketoesters is described. The compounds were investigated for their ability to form hydrogen-bonded structural networks, and for their potential interactions with the telomeric quadruplex forming sequence AGGG(TTAGGG)3.
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
, 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.
4-substituted-6-aryl-pyrimidine compounds
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, (2008/06/13)
This invention describes the synthesis and anti-neoplastic use of 4-aziridyl-5-substituted/unsubstituted 6-aryl-pyrimidine compounds of Formula IA STR1 as well as N'-[2-(1-aziridyl)ethyl]-6-aryl-2,4-pyrimidinediamines of Formula IB STR2 and 4-chloro or bromo-5-substituted/unstubstituted-6-aryl-pyrimidines.
