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  • Title: 8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
    Author: Evans GB, Furneaux RH, Gainsford GJ, Hanson JC, Kicska GA, Sauve AA, Schramm VL, Tyler PC.
    Journal: J Med Chem; 2003 Jan 02; 46(1):155-60. PubMed ID: 12502369.
    Abstract:
    The 8-aza-immucillins (8-aza-9-deazapurines linked from C9 to C1 of 1,4-dideoxy-1,4-iminoribitol) have been designed as transition-state analogues of the reactions catalyzed by purine nucleoside phosphorylase and nucleoside hydrolases. Syntheses of the 8-aza-immucillin analogues of inosine and adenosine are described. They are powerful inhibitors of the target enzymes with equilibrium dissociation constants as low as 42 pM.
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