TY - JOUR
T1 - N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists
AU - Ashton, Trent Damon
AU - Baker, Stephen P
AU - Hutchinson, Sally A
AU - Scammells, Peter John
PY - 2008
Y1 - 2008
N2 - Adenosines bearing 5 -modification in conjunction with an N-6-substituent have previously been shown to act as partial agonists at the A(1) adenosine receptor. Our current work investigates the effect of modifying the 5 -position in conjunction with efficacious bicyclic and tricyclic N-6-substituents. Several highly potent agonists for the A(1) adenosine receptor were identified; however, all of these compounds behaved as full agonists. In keeping with previous reports, 5 -halogen and 5 -sulfide derivatives of N-6-(endo-norborn-2-yl) adenosine were, in general, low nanomolar agonists of the A(1) adenosine receptor. The known partial agonist, N-6-cyclopentyl-5 -deoxy-5 -ethylthioadenosine (2), also behaved as a full agonist in our assay. (C) 2007 Elsevier Ltd. All rights reserved.
AB - Adenosines bearing 5 -modification in conjunction with an N-6-substituent have previously been shown to act as partial agonists at the A(1) adenosine receptor. Our current work investigates the effect of modifying the 5 -position in conjunction with efficacious bicyclic and tricyclic N-6-substituents. Several highly potent agonists for the A(1) adenosine receptor were identified; however, all of these compounds behaved as full agonists. In keeping with previous reports, 5 -halogen and 5 -sulfide derivatives of N-6-(endo-norborn-2-yl) adenosine were, in general, low nanomolar agonists of the A(1) adenosine receptor. The known partial agonist, N-6-cyclopentyl-5 -deoxy-5 -ethylthioadenosine (2), also behaved as a full agonist in our assay. (C) 2007 Elsevier Ltd. All rights reserved.
UR - http://www.sciencedirect.com/science/article/pii/S0968089607009789
M3 - Article
SN - 0968-0896
VL - 16
SP - 1861
EP - 1873
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
IS - 4
ER -