Antimicrobial Activities of Amine- and Guanidine-Functionalized Cholic Acid Derivatives | Antimicrobial Agents and Chemotherapy

DOI: 10.1128/AAC.43.6.1347

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Fig. 1.
Structures of cholic acid derivatives 1 to8.

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Table 1.

MICs and MBCs of cholic acid derivatives 1 to8

Organism	MIC (MBC) (μg/ml)
	Compound								PMB
	1	2	3	4	5	6	7	8	PMB
Gram-negative rods
E. coli ATCC 25922	22 (22)	5.1 (6.8)	1.4 (3.8)	80 (90)	36 (40)	6.6 (7.4)	3.0 (3.0)	0.31 (0.37)	1.8 (1.8)
K. pneumoniae ATCC 13883	24 (>36)	14 (17)	3.0 (6.7)	>100 (>100)	47 (50)	23 (27)	2.6 (5.8)	0.84 (3.0)	5.3 (6.8)
P. aeruginosa ATCC 27853	26 (38)	11 (>17)	5.9 (9.9)	85 (97)	21 (36)	4.6 (6.4)	2.0 (3.2)	2.0 (2.9)	0.20 (3.9)
S. typhimurium ATCC 14028	21 (>25)	13 (16)	2.2 (3.8)	>100 (>100)	43 (>47)	86 (90)	2.6 (6.7)	0.81 (1.8)	NM^a
Gram-positive cocci
E. faecalis ATCC 29212	4.9 (50)	3.4 (19)	2.2 (16)	12 (>100)	3.3 (19)	3.1 (4.7)	3.1 (5.5)	3.0 (5.8)	40 (>100)
S. aureus ATCC 25923	3.1 (5.7)	1.0 (4.7)	0.6 (3.2)	8.6 (54)	2.0 (9.2)	0.55 (4.2)	0.40 (2.0)	0.59 (1.4)	26 (>100)
S. pyogenes ATCC 19615	3.0 (4.4)	2.0 (2.3)	2.0 (2.1)	18 (37)	4.2 (5.8)	2.4 (3.0)	2.3 (2.9)	3.5 (3.5)	19 (16.3)
Fungus
C. albicans ATCC 90028	49 (>50)	30 (42)	11 (50)	75 (92)	14 (29)	41 (45)	31 (45)	53 (76)	NM

↵a NM, not measured.

Table 2.
MICs of erythromycin, novobiocin, and rifampin alone
Drug MIC (μg/ml) for:
E. coli ATCC 25922 K. pneumoniae ATCC 13883 P. aeruginosa ATCC 27853 S. typhimurium ATCC 14028
Erythromycin 30 33 >100 61
Novobiocin 41 75 >100 >100
Rifampin 7.6 19 26 21

Table 3.

Concentrations of compounds 1, 2,4, 5, and 6 required to lower the MIC of erythromycin and FICs of combinations

Compound	Concn and FIC for^a:
	E. coli ATCC 25922 [1.0]		K. pneumoniae ATCC 13883 [1.0]		P. aeruginosa ATCC 27853 [3.0]		S. typhimurium ATCC 14028 [1.0]
	Concn	FIC (IC_1.0)	Concn	FIC (IC_1.0)	Concn	FIC (IC_3.0)	Concn	FIC (IC_1.0)
1	2.5	0.15	1.0	0.072	6.6	<0.29	3.6	0.19
2	0.23	0.078	0.25	0.048	2.4	<0.25	2.0	0.17
4	3.2	0.073	3.6	<0.066	16	<0.22	7.1	<0.088
5	1.5	0.074	0.21	0.035	2.1	<0.13	0.87	0.037
6	0.59	0.12	0.10	0.035	1.0	<0.24	0.20	0.019

↵a All concentrations are in micrograms per milliliter. Concentrations of erythromycin are indicated in brackets.

Table 4.

Concentrations of compounds 1, 2,4, 5, and 6 required to lower the MIC of novobiocin and FICs of combinations

Compound	Concn and FIC for^a:
	E. coli ATCC 25922		K. pneumoniae ATCC 13883		P. aeruginosa ATCC 27853		S. typhimurium ATCC 14028
	Concn	FIC (IC_1.0)	Concn	FIC (IC_1.0)	Concn	FIC (IC_1.0)	Concn	FIC (IC_1.0)
1	0.35	0.041	4.7	0.21	3.9	<0.16	4.4	<0.22
2	0.33	0.089	0.49	0.048	2.9	<0.27	4.5	<0.36
4	4.7	0.084	8.9	0.10	30	<0.36	8.4	<0.094
5	0.30	0.033	0.73	0.029	5.3	<0.26	1.8	<0.052
6	0.40	0.085	0.19	0.022	0.72	<0.17	0.39	<0.015

↵a All concentrations are in micrograms per milliliter. The concentration of novobiocin used was 1.0 μg/ml.

Table 5.

Concentrations of compounds 1, 2,4, 5, and 6 required to lower the MIC of rifampin and FICs of combinations

Compound	Concn and FIC for^a:
	E. coli ATCC 25922 [0.50]		K. pneumoniae ATCC 13883 [0.50]		P. aeruginosa ATCC 27853 [1.0]		S. typhimurium ATCC 14028 [1.0]
	Concn	FIC (IC_0.5)	Concn	FIC (IC_0.5)	Concn	FIC (IC_1.0)	Concn	FIC (IC_1.0)
1	0.74	0.099	0.40	0.043	1.5	0.096	0.84	0.089
2	0.80	0.22	0.12	0.035	0.50	0.086	0.39	0.079
4	4.2	0.12	1.8	0.044	11	0.17	1.4	0.064
5	0.70	0.085	0.16	0.030	0.84	0.083	0.55	0.063
6	0.81	0.19	0.11	0.031	0.50	0.15	0.10	0.051

↵a All concentrations are in micrograms per milliliter. Concentrations of rifampin are indicated in brackets.

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