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. Author manuscript; available in PMC: 2009 Jun 8.
Published in final edited form as: ChemMedChem. 2008 Aug;3(8):1250–1268. doi: 10.1002/cmdc.200800047

Table 1.

Ba ENR inhibition and antibacterial activity for modifications of ring A.

graphic file with name nihms96579f11.jpg
Compound R1 R2 IC50 (μM) or % inhibition at 1μM MIC[b] (μg/mL)
Triclosan 0.6 ± 0.0 3.1
52 Cl graphic file with name nihms96579t1.jpg 0.5% NT
53 Cl OMe 0% NT
54 Cl NH2 4.4% NT
14 Cl CO2H 0% NT
16 Cl CH2OH 1.8% NT
17 Cl CONH2 0% NT
55 Cl OH 0.5 ± 0.1 32
1 OH OH 6.3 ± 0.4 64
2 NO2 OH >50 5.8
26 CH2CH(OH)CH2OH OH 9.8% >104
28 CH2OH OH 5.0% 43
29 CH2NHCH(CH3)CH2CH2CH3 OH 0% >109
30 CH2–(1–piperidine) OH 0% >113
31 CH2NHCH2Ph OH 7.9% >122
27 n-propyl OH >0.8[a] 22.8
[a]

Saturation with inhibitor was not obtained over the concentration range tested. The percent inhibition of BaENR showed a linear response to increasing inhibitor concentrations.

[b]

MIC values are against ΔANR B. anthracis. NT = Not tested.