299916-78-2Relevant articles and documents
PHOSPHORIBOSYLTRANSFERASE INHIBITORS AND USES THEREOF
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, (2012/11/14)
The invention relates to compounds of formula (I) that are inhibitors of hypoxanthine and/or guanine purine phosphoribosyltransferases and to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and methods of treating diseases or conditions in which it is desirable to inhibit hypoxanthine and/or guanine purine phosphoribosyltransferases. Such diseases include malaria.
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase
Evans, Gary B.,Furneaux, Richard H.,Lewandowicz, Andrzej,Schramm, Vern L.,Tyler, Peter C.
, p. 3412 - 3423 (2007/10/03)
The aza-C-nucleosides, Immucillin-H and Immucillin-G, are transition state analogue inhibitors of purine nucleoside phosphorylase, a therapeutic target for the control of T-cell proliferation. Immucillin analogues modified at the 2′-, 3′-, or 5′-positions of the azasugar moiety or at the 6-, 7-, or 8-positions of the deazapurine, as well as methylene -bridged analogues, have been synthesized and tested for their inhibition of human purine nucleoside phosphorylase. All analogues were poorer inhibitors, which reflects the superior capture of transition state features in the parent immucillins.