201211-22-5Relevant academic research and scientific papers
Adenosine deaminase inhibitors: Synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA]
Pragnacharyulu,Varkhedkar,Curtis,Chang,Abushanab
, p. 4694 - 4700 (2007/10/03)
The synthesis and biological evaluation of three classes of chain-modified derivatives of (+)-EHNA are described. Among the 5',6'-unsaturated derivatives, the Z-isomer was the most potent inhibitor of adenosine deaminase (ADA) but 3-fold less active than
Adenosine deaminase inhibitors. Synthesis and biological evaluation of aralkyladenines (ARADS)
Curtis, Mark A.,Varkhedkar, Vaibhav,Pragnacharyulu, Palle V. P.,Abushanab, Elie
, p. 1639 - 1642 (2007/10/03)
Several 9-aralkyladenines have been prepared and their ADA inhibitory activity was determined. A minimum of two carbon atoms separating the aromatic ring from the adenine-bearing carbon (C3') was found essential for potent activity.
ADENOSINE DEAMINASE INHIBITORS
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, (2008/06/13)
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 (Ki) values are in the range of 1E-7 - 1E-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
