Biomedical Engineering Reference
In-Depth Information
hydrogen bond acceptor in the binding site. On the contrary, they could provide
evidences for the specification of the pharmacophore profiles.
O
O
S
HN
N
H
3
C
O
CH
3
OH
O
8
O
CH
3
S
HN
O
N
H
3
C
OH
O
O
9
CH
3
O
S
HN
O
N
OH
H
3
C
O
O
10
CH
3
O
S
HN
O
N
H
3
C
O
O
11
Benzopyran Sulfonamides
Considering that indane could be replaced by benzopyran, Lloyd and his
co-workers suggested the benzopyran core as an acceptable scaffold for potent
K
v
1.5
blockers (compound 12,IC
50
ΒΌ
M). They explored different substitu-
ent in this scaffold, such as the amide at the 6-position of benzopyrane, the
substituent on the phenyl ring of the phenyl sulfonamide, and modifications of
the amino alcohol template, to discover several compounds with good potency of
0.11
m
