In vitro Inhibitory activity of thiazoline derivatives against Aldehyde (ALR1) and Aldose (ALR2) reductase enzymes.
| Code | Structure | ALR2 | ALR1 |
|---|---|---|---|
| IC50(μM) ± SEMa/Percent inhibition | |||
| 5a |
|
13.4% | 22.6% |
| 5b |
|
27.4% | 31.9% |
| 5c |
|
22.7% | 12.4% |
| 5d |
|
19.5% | 6.7% |
| 5e |
|
20.83% | 31.4% |
| 5f |
|
3.13 ± 1.45 | 3.24 ± 2.72 |
| 5g |
|
31.73% | 24.7% |
| 5h |
|
18% | 19.6% |
| 5i |
|
16.77% | 31.3% |
| 5j |
|
5.16% | 32.8% |
| 5k |
|
35.19% | 22.6% |
| 6a |
|
4.40 ± 1.45 | 3.29 ± 1.47 |
| 6b |
|
12.9 ± 0.39 | 4.93 ± 1.86 |
| 6c |
|
10.19 ± 1.35 | 4.07 ± 2.35 |
| 6d |
|
4.21 ± 2.35 | 11.6% |
| 6e |
|
2.18 ± 0.83 | 33.5% |
| 6f |
|
3.51 ± 2.31 | 19.7% |
| 7a |
|
5.96 ± 1.05 | 23.7% |
| 7b |
|
1.39 ± 2.21 | 23.4% |
| 7c |
|
3.14 ± 1.87 | 33.4% |
| 7d |
|
11% | 4.5% |
| 7e |
|
14% | 23.6% |
| 7f |
|
23% | 21.7% |
| 7g |
|
14.49 ± 1.49 | 3.14 ± 0.41 |
| 7h |
|
9.63 ± 1.21 | 2.94 ± 1.73 |
| 7i |
|
29.62 ± | 2.20 ± 0.92 |
| 8a |
|
13.4% | 15.6% |
| 8b |
|
37.4% | 29.4% |
| 8c |
|
6.74% | 35.4% |
| 8d |
|
31% | 18.6% |
| 8e |
|
1.52 ± 0.78 | 2.94 ± 1.34 |
| 8f |
|
4.21 ± 1.63 | 12.4% |
| 8g |
|
5.16% | 23.5% |
| 8h |
|
10.32% | 33.4% |
| 8i |
|
23.22% | 12.5% |
| 8j |
|
34.83% | 27.8% |
| Valproic acidb | — | 57.4 ± 0.89 | |
| Sorbinilb | 3.14 ± 0.02 | — | |
Half maximal inhibitory concentration.
Standard inhibitor.