TY - JOUR
T1 - XH-14 analogues as adenosine antagonists
AU - Scammells, Peter J.
AU - Baker, Stephen P.
AU - Beauglehole, Anthony R.
PY - 1998/9/1
Y1 - 1998/9/1
N2 - Analogues of the potent adenosine antagonist 5-(3'-hydroxypropyl)-7-methoxy-2-(3'-methoxy-4'-hydroxyphenyl)benzo[b]furan-3-carbaldehyde (XH-14, 1) with alternate substituents in the 2-, 5- and 7-positions have been synthesised. The affinity of these compounds for the A1adenosine receptor has been evaluated using a [3H]CPX competitive binding assay. This structure-activity study highlighted the importance of the 3-formyl and 5-(3-hydroxypropyl) moieties for high receptor affinity. Copyright (C) 1998 Elsevier Science Ltd.
AB - Analogues of the potent adenosine antagonist 5-(3'-hydroxypropyl)-7-methoxy-2-(3'-methoxy-4'-hydroxyphenyl)benzo[b]furan-3-carbaldehyde (XH-14, 1) with alternate substituents in the 2-, 5- and 7-positions have been synthesised. The affinity of these compounds for the A1adenosine receptor has been evaluated using a [3H]CPX competitive binding assay. This structure-activity study highlighted the importance of the 3-formyl and 5-(3-hydroxypropyl) moieties for high receptor affinity. Copyright (C) 1998 Elsevier Science Ltd.
KW - A adenosine receptor 1
KW - Adenosine antagonist
KW - Benzofuran
UR - http://www.scopus.com/inward/record.url?scp=0032169116&partnerID=8YFLogxK
U2 - 10.1016/S0968-0896(98)00093-5
DO - 10.1016/S0968-0896(98)00093-5
M3 - Article
C2 - 9801823
AN - SCOPUS:0032169116
VL - 6
SP - 1517
EP - 1524
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
SN - 0968-0896
IS - 9
ER -