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. 2021 May 11;11(28):17259–17282. doi: 10.1039/d1ra01716k

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 graphic file with name d1ra01716k-u38.jpg 13.4% 22.6%
5b graphic file with name d1ra01716k-u39.jpg 27.4% 31.9%
5c graphic file with name d1ra01716k-u40.jpg 22.7% 12.4%
5d graphic file with name d1ra01716k-u41.jpg 19.5% 6.7%
5e graphic file with name d1ra01716k-u42.jpg 20.83% 31.4%
5f graphic file with name d1ra01716k-u43.jpg 3.13 ± 1.45 3.24 ± 2.72
5g graphic file with name d1ra01716k-u44.jpg 31.73% 24.7%
5h graphic file with name d1ra01716k-u45.jpg 18% 19.6%
5i graphic file with name d1ra01716k-u46.jpg 16.77% 31.3%
5j graphic file with name d1ra01716k-u47.jpg 5.16% 32.8%
5k graphic file with name d1ra01716k-u48.jpg 35.19% 22.6%
6a graphic file with name d1ra01716k-u49.jpg 4.40 ± 1.45 3.29 ± 1.47
6b graphic file with name d1ra01716k-u50.jpg 12.9 ± 0.39 4.93 ± 1.86
6c graphic file with name d1ra01716k-u51.jpg 10.19 ± 1.35 4.07 ± 2.35
6d graphic file with name d1ra01716k-u52.jpg 4.21 ± 2.35 11.6%
6e graphic file with name d1ra01716k-u53.jpg 2.18 ± 0.83 33.5%
6f graphic file with name d1ra01716k-u54.jpg 3.51 ± 2.31 19.7%
7a graphic file with name d1ra01716k-u55.jpg 5.96 ± 1.05 23.7%
7b graphic file with name d1ra01716k-u56.jpg 1.39 ± 2.21 23.4%
7c graphic file with name d1ra01716k-u57.jpg 3.14 ± 1.87 33.4%
7d graphic file with name d1ra01716k-u58.jpg 11% 4.5%
7e graphic file with name d1ra01716k-u59.jpg 14% 23.6%
7f graphic file with name d1ra01716k-u60.jpg 23% 21.7%
7g graphic file with name d1ra01716k-u61.jpg 14.49 ± 1.49 3.14 ± 0.41
7h graphic file with name d1ra01716k-u62.jpg 9.63 ± 1.21 2.94 ± 1.73
7i graphic file with name d1ra01716k-u63.jpg 29.62 ± 2.20 ± 0.92
8a graphic file with name d1ra01716k-u64.jpg 13.4% 15.6%
8b graphic file with name d1ra01716k-u65.jpg 37.4% 29.4%
8c graphic file with name d1ra01716k-u66.jpg 6.74% 35.4%
8d graphic file with name d1ra01716k-u67.jpg 31% 18.6%
8e graphic file with name d1ra01716k-u68.jpg 1.52 ± 0.78 2.94 ± 1.34
8f graphic file with name d1ra01716k-u69.jpg 4.21 ± 1.63 12.4%
8g graphic file with name d1ra01716k-u70.jpg 5.16% 23.5%
8h graphic file with name d1ra01716k-u71.jpg 10.32% 33.4%
8i graphic file with name d1ra01716k-u72.jpg 23.22% 12.5%
8j graphic file with name d1ra01716k-u73.jpg 34.83% 27.8%
Valproic acidb 57.4 ± 0.89
Sorbinilb 3.14 ± 0.02
a

Half maximal inhibitory concentration.

b

Standard inhibitor.