Table 3.
The activity data of compounds 35–50 expressed as MIC (MBC or MFC) [µg/ml] and {MBC/MIC or MFC/MIC} against the reference strains of bacteria and fungi
Species | MIC (MBC/MFC) [µg/ml] and {MBC/MIC or MFC/MIC} of the tested compounds | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
35 | 36 | 37 | 38 | 39 | 40 | 41 | 42 | 43 | 44 | 45 | |
Gram-positive bacteria | |||||||||||
Staphylococcus aureus ATCC 25923 |
31.25
(62.5) {2} |
31.25
(62.5) {2} |
62.5
(62.5) {1} |
31.25
(62.5) {2} |
62.5
(125) {2} |
62.5 (1000) {16} |
62.5
(125) {2} |
125 (> 1000) {nd} |
125
(250) {2} |
31.25
(62.5) {2} |
31.25
(62.5) {2} |
Staphylococcus aureus ATCC 6538 |
31.25
(31.25) {1} |
15.62
(31.25) {2} |
31.25 (250) {8} |
31.25 (250) {8} |
62.5
(125) {2} |
62.5
(125) {2} |
62.5
(125) {2} |
125
(250) {2} |
125
(250) {2} |
31.25
(31.25) {1} |
31.25
(62.5) {2} |
Staphylococcus aureus ATCC 43300 |
500
(500) {1} |
500
(1000) {2} |
500
(1000) {2} |
500
(1000) {2} |
125 (> 1000) {nd} |
500 (> 1000) {nd} |
500 (> 1000) {nd} |
250 (> 1000) {nd} |
500
(1000) {2} |
500
(1000) {2} |
500
(1000) {2} |
Staphylococcus epidermidis ATCC 12228 |
31.25
(62.5) {2} |
15.62
(31.25) {2} |
31.25
(125) {4} |
31.25
(31.25) {1} |
31.25
(125) {4} |
31.25
(125) {4} |
31.25
(62.5) {2} |
125
(125) {1} |
62.5
(125) {2} |
31.25
(62.5) {2} |
31.25
(62.5) {2} |
Micrococcus luteus ATCC 10240 |
250
(1000) {4} |
250
(1000) {4} |
250 (> 1000) {nd} |
250 (> 1000) {nd} |
250 (> 1000) {nd} |
500 (> 1000) {nd} |
250 (> 1000) {nd} |
250 (> 1000) {nd} |
250 (> 1000) {nd} |
250 (> 1000) {nd} |
250 (> 1000) {nd} |
Bacillus subtilis ATCC 6633 |
7.81
(7.81) {1} |
3.91
(3.91) {1} |
3.91
(15.62) {4} |
7.81
(7.81) {1} |
7.81
(31.25) {4} |
7.81 (250) {32} |
7.81
(15.62) {2} |
7.81 (250) {32} |
15.62
(15.62) {1} |
7.81 (250) {32} |
3.91
(15.62) {4} |
Bacillus cereus ATCC 10876 | 15.62 (250) {16} |
15.62 (125) {8} |
7.81 (500) {64} |
15.62 (250) {16} |
15.62 (250) {16} |
31.25 (250) {16} |
15.62 (500) {32} |
62.5 (500) {8} |
62.5 (500) {8} |
31.25 (250) {8} |
15.62 (250) {16} |
Gram-negative bacteria | |||||||||||
Bordetella bronchiseptica ATCC 4617 |
31.25
(62.5) {2} |
31.25
(31.25) {1} |
31.25
(31.25) {1} |
31.25
(62.5) {2} |
62.5
(125) {2} |
62.5
(125) {2} |
62.5
(62.5) {1} |
125
(125) {1} |
125
(125) {1} |
31.25
(62.5) {2} |
31.25
(31.25) {1} |
Klebsiella pneumoniae ATCC 13883 |
15.62
(15.62) {1} |
3.91
(3.91) {1} |
7.81
(7.81) {1} |
7.81
(7.81) {1} |
15.62
(31.25) {2} |
31.25
(31.25) {1} |
31.25
(31.25) {1} |
62.5
(62.5) {1} |
62.5
(62.5) {1} |
7.81
(7.81) {1} |
15.62
(15.62) {1} |
Proteus mirabilis ATCC 12453 |
1.95
(1.95) {1} |
0.98
(1.95) {2} |
3.91
(3.91) {1} |
1.95
(1.95) {1} |
1.95
(3.91) {2} |
3.91
(7.81) {2} |
3.91
(3.91) {1} |
7.81
(7.81) {1} |
7.81
(7.81) {1} |
3.91
(3.91) {1} |
3.91
(3.91) {1} |
Salmonella typhimurium ATCC 14028 |
1.95
(1.95) {1} |
1.95
(1.95) {1} |
0.98
(0.98) {1} |
0.98
(1.95) {2} |
3.91
(3.91) {1} |
3.91
(3.91) {1} |
3.91
(3.91) {1} |
7.81
(7.81) {1} |
3.91
(3.91) {1} |
3.91
(3.91) {1} |
1.95
(1.95) {1} |
Escherichia coli ATCC 25922 |
1.95
(1.95) {1} |
0.98
(0.98) {1} |
0.98
(0.98) {1} |
0.98
(0.98) {1} |
1.95
(3.91) {2} |
3.91
(3.91) {1} |
1.95
(3.91) {2} |
3.91
(3.91) {1} |
3.91
(3.91) {1} |
1.95
(3.91) {2} |
0.98
(0.98) {1} |
Pseudomonas aeruginosa ATCC 9027 |
31.25
(62.5) {2} |
31.25
(62.5) {2} |
31.25
(62.5) {2} |
31.25
(62.5) {2} |
62.5
(250) {4} |
125
(125) {1} |
62.5
(250) {4} |
125
(250) {2} |
125
(250) {2} |
31.25
(62.5) {2} |
62.5
(62.5) {1} |
Fungi | |||||||||||
Candida albicans ATCC 2091 | – | – | – | 1000 (> 1000) {nd} |
– | – | – | 1000 (> 1000) {nd} |
1000 (> 1000) {nd} |
– | – |
Candida albicans ATCC 10231 | – | – | – | 1000 (> 1000) {nd} |
– | – | – | 1000 (> 1000) {nd} |
1000 (> 1000) {nd} |
– | – |
Candida parapsilosis ATCC 22019 | – | – | – | – | – | – | 1000 (> 1000) {nd} |
500 (> 1000) {nd} |
– | – | – |
Candida glabrata ATCC 90030 | – | – | – | – | – | – | 1000 (> 1000) {nd} |
1000 (> 1000) {nd} |
– | – | – |
Candida krusei ATCC 14243 | – | – | – | – | – | – | – | 1000 (> 1000) {nd} |
– | – | – |
Species | MIC (MBC/MFC) [µg/ml] and {MBC/MIC or MFC/MIC} of the tested compounds | MIC (MBC) [µg/ml] of reference substances | ||||||||
---|---|---|---|---|---|---|---|---|---|---|
46 | 47 | 48 | 49 | 50 | CIP/NY* | NIT | CFX | APC | PA | |
Gram-positive bacteria | ||||||||||
Staphylococcus aureus ATCC 25923 |
31.25
(62.5) {2} |
125 (1000) {8} |
62.5 (1000) {16} |
125
(250) {2} |
31.25
(62.5) {2} |
0.488 | 15.62 | 0.49 | nd | 31.25 (62.5) |
Staphylococcus aureus ATCC 6538 |
31.25
(62.5) {2} |
62.5 (500) {8} |
62.5
(125) {2} |
62.5
(250) {4} |
15.62
(31.25) {2} |
0.244 | 15.62 | 0.98 | nd | 62.5 (125) |
Staphylococcus aureus ATCC 43300 | 500 (> 1000) {nd} |
1000 (> 1000) {nd} |
500 (> 1000) {nd} |
500 (> 1000) {nd} |
250 (> 1000) {nd} |
0.244 | 7.81 | nd | nd | 62.5 (125) |
Staphylococcus epidermidis ATCC 12228 |
15.62
(31.25) {2} |
62.5
(125) {2} |
31.25
(62.5) {2} |
62.5
(250) {4} |
7.81
(31.25) {4} |
0.122 | 3.91 | 0.24 | nd | 15.62 (62.5) |
Micrococcus luteus ATCC 10240 | 250 (> 1000) {nd} |
500
(1000) {2} |
250 (> 1000) {nd} |
500 (> 1000) {nd} |
250 (> 1000) {nd} |
0.976 | 62.5 | 0.98 | nd | 125 (250) |
Bacillus subtilis ATCC 6633 |
7.81
(7.81) {1} |
7.81 (62.5) {8} |
7.81 (62.5) {8} |
31.25
(31.25) {1} |
3.91
(7.81) {2} |
0.031 | 3.91 | 15.62 | nd | 3.91 (7.81) |
Bacillus cereus ATCC 10876 | 15.62 (250) {16} |
62.5 (500) {8} |
31.25 (500) {8} |
62.5 (500) {8} |
15.62 (250) {16} |
0.061 | 7.81 | 31.25 | 62.5 | 15.62 (62.5) |
Gram-negative bacteria | ||||||||||
Bordetella bronchiseptica ATCC 4617 |
31.25
(31.25) {1} |
125
(125) {1} |
62.5
(125) {2} |
125
(250) {2} |
31.25
(31.25) {1} |
0.976 | 125 | nd | nd | 31.25 (62.5) |
Klebsiella pneumoniae ATCC 13883 |
7.81
(7.81) {1} |
62.5
(62.5) {1} |
31.25
(62.5) {2} |
62.5
(62.5) {1} |
7.81
(7.81) {1} |
0.122 | 15.62 | nd | nd | 15.62 (31.25) |
Proteus mirabilis ATCC 12453 |
1.95
(1.95) {1} |
7.81
(7.81) {1} |
3.91
(3.91) {1} |
7.81
(15.62) {2} |
1.95
(3.91) {2} |
0.030 | 62.5 | nd | nd | 1.95 (3.91) |
Salmonella typhimurium ATCC 14028 |
1.95
(1.95) {1} |
3.91
(7.81) {2} |
3.91
(7.81) {2} |
7.81
(7.81) {1} |
1.95
(3.91) {2} |
0.061 | 31.25 | nd | nd | 1.95 (3.91) |
Escherichia coli ATCC 25922 |
1.95
(1.95) {1} |
3.91
(3.91) {1} |
1.95
(3.91) {2} |
7.81
(7.81) {1} |
0.98
(1.95) {2} |
0.004 | 7.81 | nd | nd | 0.98 (1.95) |
Pseudomonas aeruginosa ATCC 9027 |
31.25
(62.5) {2} |
125
(250) {2} |
62.5
(125) {2} |
125
(250) {2} |
31.25
(62.5) {2} |
0.488 | nd | nd | nd | 31.25 (62.5) |
Fungi | ||||||||||
Candida albicans ATCC 2091 | – | – | – | – | – | 0.24* | na | na | na | na |
Candida albicans ATCC 10231 | – | – | – | – | – | 0.48* | na | na | na | na |
Candida parapsilosis ATCC 22019 | – | – | – | 1000 (> 1000) {nd} |
– | 0.24* | na | na | na | na |
Candida glabrata ATCC 90030 | – | – | – | – | – | 0.24* | na | na | na | na |
Candida krusei ATCC 14243 | – | – | – | – | – | 0.24* | na | na | na | na |
The standard compounds used as positive controls: ciprofloxacin (CIP), nitrofurantoin (NIT), cefuroxime (CFX), ampicillin (APC) and pipemidic acid (PA) for bacteria and nystatin (NY*) for fungi. Compounds with bactericidal effect (MBC/MIC ≤ 4) are marked in bold. All the experiments were repeated three times (n = 3) and representative data is presented
nd not determined, na not applicable, “–” no activity