Adenosine derivatives are the sole adenosine receptor agonists. Numerous structure-activity relationship studies have pointed out that highly potent adenosine analogs, specific for a subtype of adenosine receptor, may be obtained by N6- or 2-substitution of adenosine or by substitution of the combination of such modifications. The ribose recognition domain appears to be of prime importance to activity at adenosine receptors and 2'-hydroxy, 3'-hydroxy and 5'-hydroxy groups contribute strongly to the potency of adenosine analogs as agonists. In order to further investigate the subdomain that binds the ribose moiety, we have synthesized a series of 2'-C-methyl derivatives of A1-, A2-, and A3-selective adenosine receptor agonists. The binding data of these compounds will be presented.
2'-C-Methyl analogs of selective adenosine receptors agonists: synthesis and binding studies
FRANCHETTI, Palmarisa;CAPPELLACCI, Loredana;GRIFANTINI, Mario;
1996-01-01
Abstract
Adenosine derivatives are the sole adenosine receptor agonists. Numerous structure-activity relationship studies have pointed out that highly potent adenosine analogs, specific for a subtype of adenosine receptor, may be obtained by N6- or 2-substitution of adenosine or by substitution of the combination of such modifications. The ribose recognition domain appears to be of prime importance to activity at adenosine receptors and 2'-hydroxy, 3'-hydroxy and 5'-hydroxy groups contribute strongly to the potency of adenosine analogs as agonists. In order to further investigate the subdomain that binds the ribose moiety, we have synthesized a series of 2'-C-methyl derivatives of A1-, A2-, and A3-selective adenosine receptor agonists. The binding data of these compounds will be presented.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
