Table 1. Optimization of Benzoxazole Amide Hit and Evolution of Aza-benzoxazole Series.

^aCalculated using MarvinView6.1.7.

^bInhibition of LTA induced TNFα release in THP-1 cells.

^cNot determined.

^dIC₅₀’s not determined since the maximum IRAK4 inhibitions observed were less than 90%.

^eShown as IC₅₀ ± standard deviation (N = 2).