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. Author manuscript; available in PMC: 2011 Jan 14.
Published in final edited form as: J Med Chem. 2010 Jan 14;53(1):52–60. doi: 10.1021/jm901069a

Table 2.

Second round modifications

graphic file with name nihms153805t2.jpg Compound R1 R2 IC50 (μM)a
20 3-nitro cyclopentyl 0.063
21 3-fluoro cyclopentyl 0.079
22 3-chloro cyclopentyl 0.079
23 3-bromo cyclopentyl 0.1
24 4-fluoro cyclopentyl 0.126
25 3-methyl cyclopentyl 0.126
26 4-bromo cyclopentyl 1.122
27 3-phenyl cyclopentyl 2.239
28 3-trifluoromethy1 cyclopentyl inactive
29 3,5-difluoro cyclopentyl 0.063
30 3,5-dichloro cyclopentyl 0.398
31 3,5-difluoro 2,2-difluoroethyl 0.025
a

IC50 values were determined at NIH Chemical Genomics Center using the qHTS protocol and NCGC curve fitting software. Compounds were run in duplicate with Log IC50 standard errors ranging from 0 to 0.07.