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. Author manuscript; available in PMC: 2011 Aug 2.
Published in final edited form as: J Med Chem. 2009 Aug 27;52(16):5228–5240. doi: 10.1021/jm900611t

Table 3.

Structure and activity of 1-, 2-naphthalene and benzamides

graphic file with name nihms310703u3.jpg
compound R R′ R″ IC50 (μM)
Lead 2-Naphthyl H 2-Me 8.7 ± 0.7
5h 1-Naphthyl H 2-Me 2.3 ± 0.1
21 1-Naphthyl Me 2-Me 22.6 ± 6.9
23 1-Naphthyl H 4-NH2 24.8 ± 1.0
24 1-Naphthyl H 2-Me and 5-AcNH 0.56 ± 0.03
25 1-Naphthyl H 2-Me and 5-NH2 2.64 ± 0.04

(IC50 = enzyme inhibitory activity)