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. Author manuscript; available in PMC: 2012 Sep 10.
Published in final edited form as: J Med Chem. 2011 May 3;54(10):3661–3668. doi: 10.1021/jm101401a

Table 1.

SAR of N-phenyl ring substituents. PMI and PMM assay data are the mean of at least three determinations. See Experimental Section for assay details.

graphic file with name nihms294137t1.jpg
cmpd Ar PMI IC50
(µM)		 PMM2 IC50
(µM)
1 Ph 6.4 >20
2 2-naphthyl 9.4 >20
3 3-Me-Ph 6.0 >20
4 4-Me-Ph 5.2 >20
5 3-CF3-Ph 3.4 13.9
6 4-CF3-Ph >20 >20
7 3-Cl-Ph 4.8 >20
8 4-Cl-Ph 1.9 >20
9 3-COOMe-Ph 4.9 15.4
10 4-COOEt-Ph 7.2 >20
11 3-N(Me)2-Ph 8.5 >20
12 4-N(Me)2-Ph 1.9 13.3
13 3-I-Ph 4.3 >20
14 4-tBu-Ph 5.0 >20
15 3-OMe-Ph 3.7 >10
16 2,5-di-Me-Ph 6.6 17.9