. Author manuscript; available in PMC: 2022 Jun 10.

Published in final edited form as: J Med Chem. 2021 Apr 21;64(11):7275–7295. doi: 10.1021/acs.jmedchem.1c00168

Table 1.

Summary of MIC Values Obtained during Antibacterial Assessment for 3-Functionalized HP Analogues and Comparator Compounds, Including Several Antibiotics^a

compound	MRSA-1707	MRSA-44	MRSE 35984	VRE 700221	E.faecalis OG1RF	S. pneumoniae 6303	Mtb H37Ra	Mtb CDC1551
1	3.13	3.13	3.13	6.25	18.8^b
3	1.56^c	1.56^c	2.35^b	4.69^b	12.5^c		25	13.7
18	25		18.8^b	>50
19	1.56	1.56	2.35^b	3.13
20	2.35^b	2.35^b	2.35^b	3.13	12.5
21	0.30^b	0.30^b	0.78	1.17^b	2.35^b		6.25	3.27
22	3.13	3.13	3.13	4.69^b
23	6.25		18.8^b	18.8^b
24	0.30^b	0.30^b	1.17^b	2.35^b	9.38^b		3.13	2.31
25	4.69^b	9.38^b	18.8^b	18.8^b
26	9.38^b		>50	>50
27	0.78	1.56	3.13	3.13
28	0.15^b	0.59^b	0.59^b	1.17^b	3.13		6.25	4.37
29	0.08^b	0.08^b	0.08^b	0.10	0.30^b	0.50	6.25	1.59
30	0.08^b	0.08^b	≤0.05^d	0.08^b	0.20			3.62
31	0.59^b	1.17^b	0.10	≤0.05^d	0.08^b			0.88
32	0.15^b	0.10	0.20	0.15^b	0.78		3.13	3.01
33	0.15^b	0.20	0.78	0.78	1.17^b			1.71
34	0.59^b	0.15^b	≤0.05^d	0.08^b	0.30^b		6.25	0.80
35	0.30^b	0.20	0.10	0.15^b	0.39			3.91
36	0.59^b	1.56	0.10	0.30^b	0.78
37	0.15^b	0.78	0.30^b	0.59^b	1.56
45	0.30^b	0.30^b	0.30^b	0.39	0.78			1.69
46	6.25	6.25	4.69^b	12.5
47	2.35^b	4.69^b	2.35^b	3.13
48 (1-OHP)	50	50	37.5^b	>50	>50
49 (QAC-10)	4.69^b	2.35^b	2.35^b	2.35^b	3.13
EDTA	25	125			500
TPEN	46.9^b	46.9^b			46.9^b
vancomycin	0.39		0.78	>100	0.78
daptomycin	3.13
linezolid	12.5
streptomycin							1.32

All MIC values are reported in micromolar (μM) concentrations.

Midpoint of a twofold range in observed MIC values.

Midpoint of a fourfold range in observed MIC values.

Lowest test concentration.

The test range was 0.05–50 μM for all HPs and higher (e.g., 100 μM) for comparators. EDTA and TPEN are metal-binding agent comparators. Each MIC was determined from three to nine independent experiments.