Table 1.
Inhibition constants (Ki), rp, rp/n values for monovalent, bivalent and trivalent inhibitors along with their separation lengths.
|
|
Inhibitors |
Ki [μM] |
rp[a] |
rp/n[b] |
Length[c] |
|---|---|---|---|---|---|
|
Monovalent (n=1) |
AMB |
1,395±165.8 |
– |
– |
1.09 |
|
m‐dPEG2−AMB |
259.4±35.9 |
5.4 |
5.4 |
2.13 |
|
|
m‐dPEG4−AMB |
308.9±21.5 |
4.5 |
4.5 |
2.91 |
|
|
m‐dPEG12−AMB |
359.9±35.2 |
3.9 |
3.9 |
6.19 |
|
|
m‐dPEG24−AMB |
521.1±84.9 |
2.7 |
2.7 |
11.03 |
|
|
Bivalent (n=2) |
Pentamidine |
2.1±0.8 |
664.3 |
332.1 |
2.37 |
|
Bis‐dPEG2−AMB |
55.3±5.3 |
25.2 |
12.6 |
3.34 |
|
|
Bis‐dPEG5−AMB |
44.3±5.3 |
31.5 |
15.7 |
4.48 |
|
|
Bis‐dPEG13−AMB |
131.4±23.8 |
10.6 |
5.3 |
7.64 |
|
|
Bis‐dPEG25−AMB |
290.4±95.8 |
4.8 |
2.4 |
12.39 |
|
|
Trivalent (n=3) |
Tri‐AMB |
3.9±1.7 |
357.7 |
119.2 |
2.25 |
|
Tri‐PEG4−AMB |
50.5±14 |
27.6 |
9.2 |
5.77 |
|
|
Tri‐PEG8−AMB |
130.8±15.9 |
10.7 |
3.6 |
8.66 |
|
|
Tri‐PEG12−AMB |
241.9±34.6 |
5.8 |
1.9 |
11.40 |
[a] rp: relative potency=Ki AMB/Ki multi. [b] rp/n: relative potency/number of benzamidine units. [c] calculated planar separation lengths between benzamidine moieties measured end to end using ChemDraw (Version 19.0.1.)