Figure 4.

Structure activity relationship of compound 10 analogs with respect to IL-1β inhibition. (A) A series of compound 10 analogs were ordered containing substitutions in key groups deemed important for anti-inflammatory or antifungal activity. (B) THP1 cells were treated with 50 μM of each analog or vehicle alone (0.5% DMSO) for 1 h, followed by 20 ng of LPS for 3.5 h, and then 5 mM ATP for 30 min where indicated. Experiments were conducted in technical quadruplicate and results reported as the mean ± SD from independent experiments (n = 3). * indicates p < 0.05 using one-way ANOVA and Dunnett’s post-test. (C) C. albicans was grown in YNB medium at 30 °C for 24 h and in the presence of vehicle (0.5% DMSO) or each analog (50 μM). After incubation, wells were resuspended by pipetting, OD600 nm measured, and data expressed as percentage of vehicle treated control. Experiments were repeated in biological triplicate and are reported as mean + SD * indicates p < 0.05 using one-way ANOVA and Dunnet’s post-test.