. Author manuscript; available in PMC: 2007 Jun 29.

Published in final edited form as: Bioorg Med Chem Lett. 2006 Sep 1;16(22):5773–5777. doi: 10.1016/j.bmcl.2006.08.078

Table 2.

IC₅₀ results for a selected subset of urea compounds from Schemes 1 and 2

graphic file with name nihms21272f6.jpg

Compound	IC₅₀^a(nM)	Inhibition^b(%)	R¹	Mp (°C)
1{1}	0.5 ± 0.1	86 ± 9	Adamantyl	242–245
1{4}	0.5 ± 0.1	87 ± 8	c-Hep	158–167
1{12}	1.0 ± 0.1	76 ± 7	4-I–Ph–	198–201
1{13}	0.7 ± 0.1	81 ± 8	4-Cl–Ph	177–182
1{14}	0.6 ± 0.1	80 ± 6	4-Br–Ph	192–194
1{15}	0.9 ± 0.1	84 ± 7	4-OCF₃–Ph	157–158
1{16}	1.2 ± 0.2	82 ± 5	4-CF₃–Ph	171–174
1{34}	100 ± 5	2 ± 3	2-OCF₃–Ph	158–160
1{38}	1200 ± 100	4 ± 3	2,6-Di-Me–Ph	196–199
1{39}	940 ± 60	1 ± 1	2,6-Di-Cl–Ph	181–187
1{40}	50500 ± 500	5 ± 3	2,6-Di-i-Pr–Ph	218–222
7	2.9 ± 0.2	62 ± 13	4-CO₂Me–Ph	162–163
8	220 ± 5	nd	4-CO₂H–Ph	269–285
9	2.0 ± 0.2	72 ± 6	3-CO₂Me–Ph	116–123
10	590 ± 60	nd	3-CO₂H–Ph	240–254

nd denotes not determined.

Determined via a kinetic fluorescent assay, results are means ± SD of three separate experiments.

Determined via an end-point fluorescent assay, results are means ± SD of three separate experiments.