31281-86-4Relevant articles and documents
Synthesis and adenosine receptor affinity and potency of 8-alkynyl derivatives of adenosine
Lambertucci,Costanzi,Vittori,Volpini,Cristalli
, p. 1153 - 1157 (2001)
Adenosine derivatives bearing different (ar)alkynyl chains at the 8-position were synthesized and tested at human adenosine receptors. Binding studies showed that all compounds possess affinity for the A3 subtype in the high nM range. Moreover, guanosine 5′-O-(3-[35S]thio)triphosphate binding assay indicated that the 8-alkynyl adenosines behaved as antagonists of NECA at A3 receptors.
Identification of 8-aminoadenosine derivatives as a new class of human concentrative nucleoside transporter 2 inhibitors
Tatani, Kazuya,Hiratochi, Masahiro,Nonaka, Yoshinori,Isaji, Masayuki,Shuto, Satoshi
supporting information, p. 244 - 248 (2015/03/30)
Purine-rich foods have long been suspected as a major cause of hyperuricemia. We hypothesized that inhibition of human concentrative nucleoside transporter 2 (hCNT2) would suppress increases in serum urate levels derived from dietary purines. To test this hypothesis, the development of potent hCNT2 inhibitors was required. By modifying adenosine, an hCNT2 substrate, we successfully identified 8-aminoadenosine derivatives as a new class of hCNT2 inhibitors. Compound 12 moderately inhibited hCNT2 (IC50 = 52 ± 3.8 μM), and subsequent structure-activity relationship studies led to the discovery of compound 48 (IC50 = 0.64 ± 0.19 μM). Here we describe significant findings about structural requirements of 8-aminoadenosine derivatives for exhibiting potent hCNT2 inhibitory activity.
NOVEL ANTIBACTERIAL COMPOUNDS
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Page/Page column 17, (2012/07/14)
The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim 1. The compounds are useful in the prevention and/or treatment of bacterial infections.
