. Author manuscript; available in PMC: 2009 Dec 11.

Published in final edited form as: J Med Chem. 2008 Dec 11;51(23):7563–7573. doi: 10.1021/jm800997s

Table 3.

MIC of the 5″-Modified Neomycin Derivatives ^f

Compounds	E. coli^a	S. aureus^b	E. coli (TG1) ^c	E. coli (pSF815) ^d	E. coli (pTZ19U-3) ^e
Neomycin B	4	1	4-8	4-8	≥2000
4a	32	4-8	16	32	≥2000
4b	32	4	8-16	16	500
4c	8	2	8-16	16	≥2000
4d	32	8	8-16	32	500-1000
4e	8	1-2	16	16	≥2000
4f	8-16	2	16	16	≥2000
4g	8-16	1-2	16	16	1000
4h	16-32	4	16	32	≥2000
4i	16	2	16	16	≥2000
5a	16-32	4	8	16-32	≥2000
5b	4	2	2-4	16	8
5c	4-8	4	2-4	32	8
5d	8-16	4-8	8-16	16	≥2000
5e	8-16	1-2	16	16-32	≥2000
5f	16	1	8-16	8-16	500-1000
5g	8-16	0.5	8-16	16	≥2000
5h	16-32	0.5-1	16	16-32	≥2000
5i	16	2	8-16	16	≥2000
5j	8	1	8-16	16	≥2000
5k	16-32	2	16	32	125-250
5l	64	8	32	64	≥2000
5m	16-32	1	16	16-32	≥2000
5n	8-16	1	8-16	16	≥2000
5o	8-16	0.5-1	8	16	≥2000
5p	32	1-2	16	64	≥2000
5q	16-32	2-4	16-32	16	125-250
33	32	2-4	8-16	16-32	500

Escherichia coli (ATCC 25922),

Staphylococcus aureus (ATCC 25923),

E. coli (TG1) (aminoglycoside susceptible strain),

E. coli (TG1) (pSF815 plasmid encoded for (AAC(6′)/APH(2″)),

E. coli (TG1) (pTZ19U-3 plasmid encoded for APH(3′)-I),

Unit: μg/mL.