Adenosine deaminase inhibitors
AssigneeThe Board of Governors for Higher Education, State of Rhode Island and Providence Plantations
InventorsElie Abushanab, Palle V. P. Pragnacharyulu
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Abstract
This invention disclosed (2S,3R)-3(6-aminopurin-9-yl) aralkan-2-ols, a novel class of adenine derivatives (also called 9-aralkyladenines, ARADS), which have been shown to inhibit the enzyme adenosine deaminase at therapeutically useful levels. The relevant inhibitory constant (K.sub.i) values are in the range of 10.sup.-7 -10.sup.-10 M. These compounds with potencies in this range can reversibly inhibit ADA in an effective manner, without permanently deactivating the enzyme. ADA inhibitors that have similar biological profiles have been shown to be of therapeutic value when used to protect heart muscle against ischemic damage.
Claims12
A compound of:
- ##STR2## where n=0-4 and R is selected from the group consisting of 4--CH.sub.3 ;
- 3--CH.sub.2 CH.sub.3 ;
- 2--CH.sub.2 CH.sub.2 CH.sub.3 ;
- H;
- 3--CH.sub.3 ;
- 2--CH.sub.2 CH.sub.3 ;
- H! 2--CH.sub.3.
Dependencies are inferred from the claim text.