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. Author manuscript; available in PMC: 2013 Jul 26.
Published in final edited form as: J Med Chem. 2012 Jul 11;55(14):6342–6351. doi: 10.1021/jm300303e

Table 1. Binding of urea compounds to T. brucei MetRS by a thermal shift assay.

graphic file with name nihms-393165-t0009.jpg

Compound Ri Aromatic
ring		 R2 T. brucei
MetRS
ΔTm (°C)a
2 3,5-diCl phenyl H 7.8±0.3
4 3-Cl,5-OMe phenyl H 7.7±0.1
5 2,3,5-TriCl phenyl H 6.4±0.3
6 3-Cl phenyl H 5.5±0.1
7 3-OMe phenyl H 4.7±0.1
8 3-OEt phenyl H 2.7±i.3
9 4-Cl phenyl H 2.5±0.i
10 2-Cl phenyl H 1.9±0.2
11 4-OMe phenyl H 1.1±0.3
12 2-OEt phenyl H 1.1±0.3
13 H phenyl H 1.3±0.1
14 2-OMe phenyl H 1.1±0.1
15 4-OEt phenyl H 0.5±0.2
16 3,5-diCl Phenyl 2-OH 8.4±0.3
17 3,5-diCl Phenyl 3-OH 7.7±0.i
18 3,5-diCl Phenyl 3-F 7.7±0.i
19 3,5-diCl phenyl 2-F 7.3±0.i
20 3,5-diCl Phenyl 4-F 6.3±0.5
21 3,5-diCl Phenyl 4-Cl 5.7±0.2
22 3,5-diCl Phenyl 3-Cl 5.2±0.3
23 3,5-diCl Phenyl 4-OH 5.8±0.3
24 3,5-diCl Phenyl 2-NH2 4.7±0.2
25 3,5-diCl phenyl 3-NH2 4.3±0.2
26 3,5-diCl 3-thiophene H 8.3±0.9
27 3-Cl,5-OMe 3-thiophene H 7.9±0.i
28 3,5-diCl 2-thiophene H 7.6±0.3
29 3,5-diCl 3-pyridine H 7.1±0.1
30 3,5-diCl 2-pyridine H 4.5±0.2
31 3,5-diCl 4-pyridine H 3.1±0.1
a

ΔTm values are the average of three independent runs.