Table 6.

Activity and cytotoxicity of T3SS inhibitors with varying substituents on the benzylamine.

Compound #	Ar	secretion IC50 (µM)	translocation IC50 (µM)	translocation CC50 (µM)
1	3,4-methylenedioxyphenyl	7.8 ± 2.0	11.1 ± 2.3	>100
2	4-fluorophenyl	9.8 ± 2.9	6.7 ± 1.0	59 ± 16
34a	phenyl	11 ± 3	12 ± 7	95 ± 21
34b	3-fluorophenyl	15 ± 3	>27	27 ± 1
34c	2-fluorophenyl	6.3 ± 1.4	8.3 ± 3.0	47± 2
34d	4-chlorophenyl	8.5 ± 2.6	>39	39 ± 8
34e	3-chlorophenyl	9.6 ± 4.1	>19	19 ± 10
34f	2-chlorophenyl	9.2 ± 2.6	9.7 ± 4.2	>100
34g	4-methylphenyl	8.1 ± 1.8	>25	25 ± 7
34h	3-methylphenyl	8.5 ± 0.1	>45	45 ± 7
34i	2-methylphenyl	11 ± 1	>100	>100
34j	4-methoxyphenyl	12 ± 5	23 ± 10	71 ± 2
34k	3-methoxyphenyl	16 ± 7	>100	>100
34l	2-methoxyphenyl	28 ± 5	n.d.	n.d.
34m	3,4-dimethoxyphenyl	22 ± 2	>36	36 ± 6
34n	2,4-dimethoxyphenyl	19 ± 4	>100	>100
34o	benzothiophene-5-yl	6.0 ± 1.6	5.3 ± 3.7	30 ± 11
34p	benzofuran-5-yl	3.7 ± 1.6	>11	11 ± 5
34q	benzimidazole-5-yl	11 ± 5	33 ± 8	62 ± 7
34r	indole-5-yl	2.1 ± 0.6	4.8 ± 0.4	>100
34s	indole-6-yl	1.9 ± 0.3	5.7 ± 0.6	9.4 ± 3.6
34t	indole-4-yl	4.8 ± 1.2	4.3 ± 2.3	24 ± 2
34u	indole-2-yl	8.9 ± 0.2	>12	12 ± 4
34v	1-methylindole-5-yl	5.1 ± 1.4	>6.3	6.3 ± 2.6
34w	pyrrolo[2,3-b]pyridin-5-yl	9.5 ± 1.3	>21	21 ± 4
34x	6-fluoropyridin-3-yl	58 ± 20	>100	>100
34y	5-fluoropyridin-2-yl	41 ± 18	>100	>100

n.d.: value not determined