Table 1. Structures and activities of reutericyclin analogs.
Number | MIC (μg/ml) against Gram-positive bacteria | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
R1 | R2CO | R3 | EF | SP | SPn | BA | BS | CD | MSSA | MRSA | |
1 | CH3 | 0.20 | 6.25 | 3.13 | 0.20 | 0.39 | 0.09 | 0.78 | 0.4 | ||
2 | ” | H | ” | >200 | >200 | >200 | >200 | >200 | >128 | >200 | >200 |
3 | ” | ” | 50 | 12.5 | 6.25 | >200 | 100 | 16 | 50 | 12.5 | |
4 | ” | ” | 12.5 | 25 | 3.13 | >200 | 25 | 8 | 12.5 | 1.6 | |
5 | ” | ” | 0.78 | 3.13 | 0.78 | >200 | 1.56 | 0.25 | 0.78 | <0.1 | |
6 | ” | (CH2)CH3 | 0.20 | 3.13 | 3.13 | 0.39 | 0.39 | <0.03 | <0.1 | <0.1 | |
7 | ” | ” | 0.39 | 12.5 | 12.5 | >200 | 0.78 | 0.75 | <0.1 | <0.1 | |
8 | ” | ” | 50 | 100 | 25 | 50 | 100 | 0.5 | 25 | 12.5 | |
9 | ” | ” | 50 | 100 | 50 | 12.5 | 12.5 | 8 | 50 | 50 | |
10 | ” | ” | 0.39 | 3.13 | 3.13 | 0.78 | 1.56 | 0.25 | 0.40 | 0.2 | |
11 | ” | ” | 0.78 | 25 | 12.5 | 0.20 | 1.56 | 0.25 | 0.78 | 0.2 | |
12 | ” | ” | 12.5 | 50 | 50 | 0.78 | 3.13 | 2 | 6.25 | 6.25 | |
13 | ” | ” | 0.20 | 6.25 | 12.5 | 0.39 | 0.39 | <0.03 | 0.20 | <0.1 | |
14 | H | ” | CH3 | 6.25 | 50 | 12.5 | 1.56 | 12.5 | 2 | 12.5 | 3.2 |
15 | ” | ” | 100 | 50 | 100 | >200 | 200 | 64 | >200 | >200 | |
16 | ” | ” | 25 | 50 | 25 | >200 | 50 | >64 | >200 | >200 | |
17 | ” | ” | 50 | >200 | >200 | >200 | >200 | >64 | 100 | 200 | |
18 | ” | ” | 6.25 | 25 | 12.5 | >200 | 12.5 | 4 | 6.25 | 0.8 | |
19 | ” | ” | 50 | 50 | 25 | 200 | 50 | 32 | 50 | 25 | |
20 | ” | ” | 0.78 | 12.5 | 6.25 | 200 | 1.56 | 0.25 | <0.1 | <0.1 |
Abbreviations: EF - Enterococcus faecalis ATCC 33186, SP - Streptococcus pyogenes ATCC 700294, SPn - Streptococcus pneumoniae R6, BA - Bacillus anthracis sterne, BS - Bacillus subtilis ATCC 23857, CD - Clostridium difficile BAA 1803, MSSA - methicillin-susceptible Staphylococcus aureus Newman, MRSA – methicillin-resistant Staphylococcus aureus N315.