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. Author manuscript; available in PMC: 2014 Nov 1.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Sep 5;23(21):10.1016/j.bmcl.2013.08.103. doi: 10.1016/j.bmcl.2013.08.103

Table 1.

Favored positioning of Ar2 substituent(s)

graphic file with name nihms522599u1.jpg
Compound R LASV EC50 (nM)
3a H 47
3b 2-Cl 320
3c 4-Cl 20
3d 3-Br 56
3e 4-Br 470
3f 3-NO2 250
3g 4-NO2 62
3h 2-OH 570
3i 3-OH 94
3j 4-OH 2.3
3k 3-OMe 42
3l 4-OMe 4.0
3m 3-Me 58
3n 4-Me 9.0
3o 2,3-diMe 800
3p 2,4-diMe 170
3q 3,4-diMe 3.9
3r 3,4-diCl 72
3s 3,4-diOMe 450
3t 4-cyclohexyl 24
3u 4-phenyl 1.3
3v 4-NHAc 2.6
3w graphic file with name nihms522599t1.jpg 2.1
3x graphic file with name nihms522599t2.jpg 6300
3y graphic file with name nihms522599t3.jpg 0.95
3z graphic file with name nihms522599t4.jpg 0.34