Biomedical Engineering Reference
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were synthesized and introduced into cationic lipids applying the
concept of “Libraries from Libraries,” (Fig. 1.10) [21].
O
N
H
N
N
H
N
N
H
H
H
N
O
2
N
N
H
H
RPR-204014
N
H
O
H
N
N
2
N
H
N
N
N
H
H
O
RPR-204026
H
N
O
H
N
N
H
2
N
H
N
H
N
N
N
H
H
N
O
H
N
2
O
RPR203900
H
N
H
2
N
N
N
N
H
N
N
N
H
N
H
N
H
H
O
N
H
2
H
H
N
N
N
2
RPR205856
H
N
H
H
N
2
H
N
O
O
N
H
N
H
O
H
O
H
N
N
B
o
c
N
H
N
B
o
c
N
B
o
c
B
o
c
H
N
B
o
c
H
N
N
B
o
c
N
B
o
c
N
B
o
c
N
B
o
c
B
o
c
H
N
S
trifluoroethanol
trifluoroethanol
B
o
c
N
N
H
B
o
c
H
N
N
H
H
N
N
2
2
H
O
H
N
N
H
O
2
2
Br
H
N
N
H
2
2
N
N
N
H
Cl
2
H
N
N
2
N
H
S
S
2
B
o
c
N
N
H
B
o
c
B
o
c
N
N
H
B
o
c
H
N
H
N
trifluoroethanol
N
H
B
o
c
O
N
B
o
c
N
B
o
c
B
o
c
H
N
H
N
O
H
N
B
o
c
N
B
o
c
H
N
N
N
N
B
o
c
O
H
B
o
c
H
N
N
B
o
c
N
B
o
c
H
N
O
N
B
o
c
H
N
B
o
c
H
N
Figure 1.10
Synthesis of geometrically varied mono-functionalized
poly(amino)-guanidine building blocks on solid phase
(Libraries from libraries) and geometrically varied lipo-
poly-guanidinium-amines containing the synthetic building
blocks.
Finally, we have developed a family of cyclic polyaminoguani-
dines. Again a combinatorial approach applying the concept of
libraries from libraries generated on solid support of a variety of
building blocks that were introduced into lipids (Fig. 1.11). Some of
the products have been found to be useful for intramuscular gene
delivery and to be more efficient than naked DNA [33].
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