TABLE 2

Inhibition of PA-Nter by different DKA or DKA-bioisosteric indole derivatives as determined in the plasmid-based enzymatic assay

One microgram of PA-Nter was incubated with 1 μg of M13mp18 plasmid substrate and the compounds. After 2 hours incubation, cleavage was assessed by gel electrophoresis.

Compound	R₁	R₂	IC₅₀
			μM
30	H	Me	3.4
31	H	Bn	22
32	Me	Me	10
33	Me	Et	4.1
34	H	Me	0.6
35	H	Et	5.5
36	H	Bn	8.9
37	Me	Bn	204
38	Me	Me	21
39	H	Me	0.6
40	H	Et	0.8
41	H	Bn	1.6
42	H	Me	3.5
43	Me	Me	22
44	—	Et	>500
45	H	H	>500
46	Me	H	>500
47	Me	Ph	>500