TY - JOUR
T1 - Ring-constrained (N)-methanocarba nucleosides as adenosine receptor agonists
T2 - Independent 5′-uronamide and 2′-deoxy modifications
AU - Lee, Kyeong
AU - Ravi, Gnana
AU - Ji, Xiao Duo
AU - Marquez, Victor E.
AU - Jacobson, Kenneth A.
PY - 2001/5/21
Y1 - 2001/5/21
N2 - Novel methanocarba adenosine analogues, having the pseudo-ribose northern (N) conformation preferred at adenosine receptors (ARs), were synthesized and tested in binding assays. The 5′-uronamide modification preserved [N6-(3-iodobenzyl)] or enhanced (N6-methyl) affinity at A3ARs, while the 2′-deoxy modification reduced affinity and efficacy in a functional assay.
AB - Novel methanocarba adenosine analogues, having the pseudo-ribose northern (N) conformation preferred at adenosine receptors (ARs), were synthesized and tested in binding assays. The 5′-uronamide modification preserved [N6-(3-iodobenzyl)] or enhanced (N6-methyl) affinity at A3ARs, while the 2′-deoxy modification reduced affinity and efficacy in a functional assay.
UR - https://www.scopus.com/pages/publications/0035927233
U2 - 10.1016/S0960-894X(01)00213-X
DO - 10.1016/S0960-894X(01)00213-X
M3 - Article
C2 - 11392549
AN - SCOPUS:0035927233
SN - 0960-894X
VL - 11
SP - 1333
EP - 1337
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 10
ER -