Table 3.

Antibacterial activity (minimal inhibitory concentration, MIC) of compounds 1a-s, 2a-s, 4 and ciprofloxacin (positive control) against the ESKAPE panel of pathogens (E1 = Enterococcus faecium (G+), S = Staphylococcus aureus (G+), K = Klebsiella pneumonia (G-), A = Acinetobacter baumannii (G-), P = Pseudomonas aeruginosa (G-), E2 = Enterobacter aerogenes (G-)).

Entry	Compound	R1NR2 Side Chain	MIC, μg/mL
			E1	S	K	A	P	E2
1	1a		16	>100	>100	16	>100	>100
2	2a		8	63	8	>100	>100	63
3	1b		8	>100	>100	4	>100	>100
4	2b		8	>100	2	2	>100	8
5	1c		16	>100	>100	4	>100	>100
6	2c		63	>100	>100	8	>100	>100
7	1d		8	16	32	>100	>100	63
8	2d		8	63	16	>100	>100	63
9	1e		4	>100	63	>100	>100	>100
10	2e		8	8	>100	4	>100	63
11	1f		4	>100	>100	8	>100	>100
12	2f		8	63	8	32	>100	16
13	1g		4	>100	>100	32	>100	>100
14	2g		32	>100	>100	8	>100	63
15	1h		16	>100	>100	32	>100	>100
16	2h		4	16	>100	63	>100	>100
17	1i		2	4	32	32	>100	32
18	2i		2	>100	>100	>100	>100	>100
19	1j		4	>100	>100	4	>100	>100
20	2j		8	>100	>100	63	>100	>100
21	1k		2	63	>100	>100	>100	>100
22	2k		>100	>100	>100	4	>100	>100
23	1l		63	>100	>100	4	>100	>100
24	2l		16	16	>100	8	>100	>100
25	1m		8	8	32	2	>100	16
26	2m		16	>100	>100	8	>100	>100
27	1n		>100	>100	>100	>100	>100	>100
28	2n		4	32	>100	63	>100	>100
29	1o		2	4	16	32	>100	32
30	2o		>100	>100	>100	8	>100	>100
31	1p		32	>100	>100	8	>100	>100
32	2p		4	>100	>100	8	>100	>100
33	1q		16	>100	>100	4	>100	>100
34	2q		32	63	>100	16	>100	>100
35	1r		16	>100	>100	8	>100	63
36	2r		16	63	>100	>100	>100	>100
37	1s		16	63	63	>100	>100	>100
38	2s		2	>100	>100	4	>100	>100
39	4		32	>100	>100	>100	>100	>100
40	ciprofloxacin		0.3	1.25	0.6	2.5	0.6	1.25

* Attachment to position 4 in triazolopyrimidine scaffold (compounds 1) or position 2 (compounds 2).