Table 3.

MIC assays on engineered (EC) and clinical (AG) strains of E. coli bearing specific resistance determinants (MIC, μg/mL) ^[a]

		Engineered (EC) Strains					Clinical (AG) Strains
		EC026	EC189	EC191	EC125	EC141	AG212	AG163	AG166
Compound	4”-Substituent	wt	APH(3’)-Ia	APH(3’)-IIa	APH(3’)-IIb	APH(3’)-VI	wt	APH(3’)-I	APH(3’)-II
Neomycin series (6 basic amines in parent)
Neomycin, 4	CH2OH	1	32–64	16–32	16–32	8–16	1	64–128	64–128
27	H	1	128	≥128	128	64–128	1–2	>128	>128
31	CH3	1	≥128	>128	128	64–128	2	>128	>128
34	CH2NH2	1–2	64–128	32	32	16–32	2–4	128	128
35	CH2NHCHO	1	8–16	16	8–16	16	1–2	32–64	64
36	CH2NHAc	0.5–1	≥128	≥128	128	128	1–2	>128	>128
Paromomycin series (5 basic amines in parent)
Paromomycin, 3	CH2OH	1	>128	32–64	64–128	64	2–4	>128	>128
40	H	4	>64	>64	>64	>64	16	>128	>128
46	CH3	16	>128	>128	>128	>128	32	>128	>128
49	CH2NH2	4	16–32	16–32	32	16–32	4	>64	>64
51	CH2NHCHO	1	8–16	32	64	32–64	2–4	64	>128
52	CH2NHAc	4–8	>128	>128	>128	>128	16	>128	>128
53	CH2NHCONH2	2	32	32–64	>32	>32	4–8	>128	>128
Propylamycin series (5 basic amines in parent)
Propylamycin, 19	CH2OH	0.25–0.5	64–128	0.5–1	0.5–1	0.5	1	>128	1–2
20	CH2NH2	0.5–1	2–4	1–2	0.5–1	0.5–1	2–4	16	2–4
21	CH2NHCHO	0.5–1	2	0.5–1	0.5	0.25	1–2	4–8	2–4
22	CH2NHCONH2	1	8	2–4	2	0.5–1	4	32	16–32
Ribostamycin series (4 basic amines in parent)
Ribostamycin, 6	CH2OH	1–2	>128	>128	>128	>128	4	>128	>128
57	H	16	>128	>128	>128	>128	64	>128	>128
64	CH2NH2	-	-	-	-	-	8	>128	>128
66	CH2NHCHO	4	>128	>128	>128	>128	16	>128	>128
67	CH2NHAc	16–32	>128	>128	>128	>128	64–128	>128	>128
Apralog series (5 basic amines in parent)
14	CH2OH	1–2	1–2	1	1	1	4–8	8	4–8
15	H	2	1–2	1	1	1	8	8	8
79	CH3	2–4	4–8	2–4	2–4	2–4	8–16	8–16	8–16
16	CH2NH2	1–2	1	1	1	1	4	2	8
75	CH2NHCHO	2–4	-	-	-	-	8	16	8–16
Advanced Apralog series (6 basic amines in parent)
17	CH2OH	0.5–1	0.5–1	0.5	0.5	0.5	2	4	2
18	CH2NH2	0.25–0.5	0.5–1	0.5	0.25	0.5	1–2	1–2	2
76	CH2NHCHO	0.5–1	0.5–1	0.25–0.5	0.25	0.25–0.5	2–4	2–4	2–4

^[a]All values were determined in at least duplicate using 2-fold dilution series