Table 2.
Kinetic parameters of α-aminoalkylphosphonate diaryl ester peptidyl derivatives
No. | Structure | log EC50 [µM] |
EC50 [µM] | Ki [µM] |
% Inh (50 µM) |
||
---|---|---|---|---|---|---|---|
![]() | |||||||
R 1 | R 2 | R 3 | |||||
23 | -CH(CH3)2 | -CH3 | -CH2CH3 | 1.535 ± 0.031 | 34.25 | 17.00 | 64.1 |
24 | -CH(CH2)5 | -CH3 | -CH2CH3 | 1.313 ± 0.053 | 20.54 | 10.19 | 74.1 |
25 | -CH(CH3)2 | -CH3 | -CH(CH3)2 | 1.342 ± 0.026 | 21.98 | 10.90 | 81.8 |
26 | -CH(CH2)5 | -CH3 | -CH(CH3)2 | 1.297 ± 0.033 | 19.83 | 9.84 | 85.8 |
27 | -CH(CH3)2 | -CH3 | -C(CH3)3 | 1.328 ± 0.039 | 21.26 | 10.54 | 83.3 |
28 | -CH(CH2)5 | -CH3 | -C(CH3)3 | 1.427 ± 0.041 | 26.76 | 13.27 | 77.3 |
29 | -CH(CH3)2 | -CH3 | -H | 1.503 ± 0.042 | 31.86 | 15.81 | 62.1 |
30 | -CH(CH2)5 | -CH3 | -H | 1.481 ± 0.060 | 30.24 | 15.00 | 69.0 |
31 | -CH(CH3)2 | -CH2CH3 | -H | 1.580 ± 0.056 | 37.97 | 18.84 | 57.0 |
32 | -CH(CH2)5 | -CH2CH3 | -H | 1.380 ± 0.074 | 23.97 | 11.89 | 71.0 |
33 | -CH(CH3)2 | -CH(CH3)2 | -H | 1.543 ± 0.052 | 34.96 | 17.35 | 58.5 |
34 | -CH(CH2)5 | -CH(CH3)2 | -H | 1.378 ± 0.034 | 23.85 | 11.83 | 70.5 |
35 | -CH(CH3)2 | -CH(CH3)CH2CH3 | -H | 1.251 ± 0.037 | 17.84 | 8.84 | 77.4 |
36 | -CH(CH2)5 | -CH(CH3)CH2CH3 | -H | 1.211 ± 0.036 | 16.24 | 8.05 | 81.4 |
37 | -CH(CH3)2 | -CH2CH(CH3)2 | -H | 1.449 ± 0.062 | 28.13 | 13.96 | 67.4 |
38 | -CH(CH2)5 | -CH2CH(CH3)2 | -H | 1.026 ± 0.051 | 10.61 | 5.25 | 84.2 |
39 | -CH(CH3)2 | -CH2CH2SCH3 | -H | 1.418 ± 0.041 | 26.20 | 13.00 | 65.8 |
40 | -CH(CH2)5 | -CH2CH2SCH3 | -H | 1.420 ± 0.028 | 26.31 | 13.05 | 73.8 |
41 | -CH(CH3)2 | -CH2(C6H5) | -H | -0.884 ± 0.036 | 0.13 | 0.05 | 100.0 |
42 | -CH(CH 2 ) 5 | -CH2(C6H5) | -H | -0.132 ± 0.034 | 0.74 | 0.35 | 100.0 |
43 | -CH(CH3)2 | -CH2CH2(C6H5) | -H | 1.235 ± 0.048 | 17.17 | 13.00 | 85.4 |
44 | -CH(CH2)5 | -CH2CH2(C6H5) | -H | 1.184 ± 0.046 | 15.27 | 7.57 | 86.5 |