Table 5.

Activity and cytotoxicity of T3SS inhibitors with amide linker modifications.

Compound #	L	secretion IC50 (µM)	translocation IC50 (µM)	translocation CC50 (µM)
2	−NHCH2-	9.8 ± 2.9	6.7 ± 1.0	59 ± 16
28a	−NH-	>100	n.d.	n.d.
28b	−NHCH2CH2-	12 ± 4	>17	17 ± 11
28c	−NHCH2CH2CH2-	>100	n.d.	n.d.
28d	−N(Me)CH2-	28.5 +/−10.6	n.d.	n.d.
29a	−OCH2-	>100	n.d.	n.d.
29b	−OCH2CH2-	>100	n.d.	n.d.
30a	−NHNH-	47 ± 7	23 ± 4	35 ± 2
30b	−NHNHCH2-	4.3 ± 0.6	8.3 ± 2.3	31 ± 1
31	−NHOCH2-	4.0 ± 0.3	24 ± 7	59 ± 15
33	−CH2CH2-	>100	n.d.	n.d.

n.d.: value not determined