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. 2022 Apr 22;27(9):2696. doi: 10.3390/molecules27092696

Table 1.

The inhibitory effects of 2,5-diaminobenzoxazole derivatives on IL-6/STAT3 signaling and production of IL-1β from macrophages.

graphic file with name molecules-27-02696-i001.jpg
Compound R1 R2 R3 R4 IL-6/STAT3 Inhibition (%)
(10 μg/mL)
IL-1β Production Inhibition (%)
(10 μg/mL)
NO LPS 100.0 ± 0.5 100.0 ± 4.1
LPS 0.0 ± 4.9 0.0 ± 7.4
3a H OCH3 H H 29.3 ± 4.7 ** 92.1 ± 4.5 **
3b H OCH2CH3 H H 59.1 ± 6.5 ** 76.5 ± 2.2 **
3c H CH3 H H 17.0 ± 19.7 * 13.7 ± 1.4 *
3d H CH(CH3)2 H H 65.9 ± 7.2 ** 75.3 ± 4.7 **
3e H (CH2)3CH3 H H 71.5 ± 8.2 ** 74.4 ± 8.1 **
3f Br H H H 58.0 ± 5.1 ** 79.8 ± 1.4 **
4a H CH2CH3 H CH3 35.9 ± 7.2 ** 88.2 ± 6.7 **
4b H CH2CH3 H COCH3 34.4 ± 8.7 ** 54.5 ± 4.8 **
4c H CH2CH3 H COCH(CH3)2 13.0 ± 0.4 * 88.1 ± 2.2 **
4d H CH2CH3 H COCH2OCH3 9.6 ± 2.6 * 26.6 ± 1.0 **
Madindoline 52.0 ± 4.6 **

* p < 0.05, ** p < 0.01 vs. LPS inhibition (%). Data are presented as the mean ± SD. Student’s t-test was used for comparisons involving two groups (n = 3).