Table 2.

Antibacterial Activity Against Relevant Pathogens (MIC, μg/mL)^[a]

	Strain	AG212	AG215	AG290	AG225	AG220	AG038
Compound	4”-Substituent	E. coli	K. pneumoniae	E. cloacae	A. baumanii	P. aeruginosa	MRSA
Neomycin series (6 basic amines in parent)
Neomycin, 4	CH2OH	1	0.5	1	1–2	32–64	1
27	H	1–2	0.5–1	1–2	2–4	>64	1
31	CH3	2	1–2	1–2	2–4	>64	1–2
34	CH2NH2	2–4	2	2–4	8	16–32	1–2
35	CH2NHCHO	1–2	0.5–1	1	2–4	64	1–2
36	CH2NHAc	1–2	0.5–1	1–2	2–4	>64	1
Paromomycin series (5 basic amines in parent)
Paromomycin, 3	CH2OH	2–4	1	2	2–4	>64	2
40	H	16	4–8	8–16	16	>64	8
46	CH3	32	16	32	64	>64	16–32
49	CH2NH2	4	2–4	4	4	>64	2–4
51	CH2NHCHO	2–4	1	2	2–4	>64	2–4
52	CH2NHAc	16	8	8–16	8–16	>64	8
53	CH2NHCONH2	4–8	2	2–4	4–8	>64	2–4
Propylamycin series (5 basic amines in parent)
Propylamycin, 19	CH2OH	1	0.25–0.5	0.5	1–2	8	1–2
20	CH2NH2	2–4	1	1	2	4	2
21	CH2NHCHO	1–2	1	1	2	8	1–2
22	CH2NHCONH2	4	2–4	2–4	2–4	>64	2–4
Ribostamycin series (4 basic amines in parent)
Ribostamycin, 6	CH2OH	4	2	2–4	4	>128	4
57	H	64	32	64	64	>128	32
64	CH2NH2	8	4	4	4	>32	8
66	CH2NHCHO	16	8	8–16	16	>128	16–32
67	CH2NHAc	64–128	32	64	128	>128	64–128
Apralog series (5 basic amines in parent)
14	CH2OH	4–8	1–2	2–4	8–16	32–64	4–8
15	H	8	2–4	2–4	8	16–32	2–4
79	CH3	8–16	8	8–16	16	64	4
16	CH2NH2	4	1–2	2	8	4–8	2
75	CH2NHCHO	8	2–4	4–8	16	>64	8–16
Advanced Apralog series (6 basic amines in parent)
17	CH2OH	2	1–2	1–2	4–8	16	2–4
18	CH2NH2	1–2	0.5–1	1	2	2	1–2
76	CH2NHCHO	2–4	1	1–2	4–8	16–32	4

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