152529-70-9Relevant articles and documents
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A1receptor antagonists and their biological evaluation
Koul, Summon,Ramdas, Vidya,Barawkar, Dinesh A.,Waman, Yogesh B.,Prasad, Neela,Madadi, Santosh Kumar,Shejul, Yogesh D.,Bonagiri, Rajesh,Basu, Sujay,Menon, Suraj,Reddy, Srinivasa B.,Chaturvedi, Sandhya,Chennamaneni, Srinivas Rao,Bedse, Gaurav,Thakare, Rhishikesh,Gundu, Jayasagar,Chaudhary, Sumit,De, Siddhartha,Meru, Ashwinkumar V.,Palle, Venkata,Chugh, Anita,Mookhtiar, Kasim A.
, p. 1963 - 1975 (2017/03/09)
Multipronged approach was used to synthesize a library of diverse C-8 cyclopentyl hypoxanthine analogs from a common intermediate III. Several potent and selective compounds were identified and evaluated for pharmacokinetic (PK) properties in Wistar rats. One of the compounds 14 with acceptable PK parameters was selected for testing in in vivo primary acute diuresis model. The compound demonstrated significant diuretic activity in this model.
SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS, ITS PREPARATION AND USES THEREOF
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Page/Page column 49-50, (2011/06/11)
The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating co
Synthesis of Paraxanthine Analogs (1,7-Disubstituted Xanthines) and Other Xanthines Unsubstituted at the 3-Position: Structure-Activity Relationships at Adenosine Receptors
Mueller, Christa E.,Shi, Dan,Manning, Malcolm,Daly, John W.
, p. 3341 - 3349 (2007/10/02)
Synthetic procedures for the preparation of various 3-unsubstituted xanthines, including paraxanthine analogs (1,7-disubstituted xanthines) and 1,8-disubstituted xanthines, were developed.Sylylation of 1-substituted xanthines followed by alkylation at the 7-position provides a facile route to paraxanthine analogs.Regioselective alkylation of tris(trimethylsilyl)-6-aminouracil provides 3-substituted 6-aminouracils, which are converted to 1,8-disubstituted xanthines by standard procedures.The ring closure of 3-substituted 5-cyclopentanecarboxamido- and 5-(benzoylamino)-6-aminouracils requires drastic reaction conditions.Affinity for brain A1 and A2 adenosine receptors was determined in binding assays for these and other xanthines with substituents in 1-, 3-, 7-, 8-, and 9-positions.Substitution at the 1-position was necessary for high affinity at adenosine receptors. 1,3-Disubstituted xanthines generally had higher affinity than 1,7-disubstituted xanthines. 1,8-Disubstituted xanthines had high affinity for adenosine receptors; some were highly selective for A1 receptors.