Table 1.
| |||||
---|---|---|---|---|---|
KIa |
|||||
No. | R | R1 | hCA I (nM) | hCA II(nM) | MgCA (µM) |
1b | H | 891 | 26.7 | 14.1 | |
2b | H | >2000 | 43.7 | 18.9 | |
3b | H | >2000 | 35.0 | 7.81 | |
4b | n-Pr | n-Pr | >2000 | 46.7 | 1.85 |
5b | n-Bu | n-Bu | 909 | >2000 | 7.52 |
6b | i-Bu | i-Bu | 681 | 43.0 | 8.61 |
7b | Et | n-Bu | 700 | >2000 | 5.26 |
8b | Me | 827 | 44.5 | 9.16 | |
9b | Me | Bn | >2000 | >2000 | 7.61 |
10b | –(CH2CH2)–O–(CH2CH2)– | 569 | >2000 | 7.65 | |
11b | –(CH2CH2)–NH–(CH2CH2)– | 876 | 22.4 | 7.41 | |
12b | –(CH2CH2)–N(4–F–C6H4)–(CH2CH2)– | 895 | 46.8 | 8.33 | |
13b | –(CH2CH2)–N(4–CF3–C6H4)–(CH2CH2)– | >2000 | 43.6 | 4.22 | |
14b | –(CH2CH2)–N(3–Cl–C6H4)–(CH2CH2)– | 686 | >2000 | 15.9 | |
15b | –(CH2CH2)–N(CH2CONHC6H11)–(CH2CH2)– | 949 | 45.9 | 6.13 | |
16b | Bn | – | 4.1 | 0.70 | 8.12 |
17b | – | 64.1 | 5.4 | 16.2 | |
AAZ | 250 | 12 | 74 |
Mean from three different assays, by a stopped flow technique (errors were in the range of ±5–10% of the reported values); bhCA I and hCA II data from Ref.14f.