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. Author manuscript; available in PMC: 2012 May 17.
Published in final edited form as: J Am Chem Soc. 2011 Jul 21;133(32):12834–12841. doi: 10.1021/ja204969m

Table 2. Effect of ring size on potency of spirane amine inhibitors against WT A/M2 and A/M2-V27A.

Compound Structure IC50 WT A/M2 (μM) IC50A/M2-V27A (μM)
6 graphic file with name nihms373510t6.jpg 3.3 ± 0.2 319.1 ± 57.4
3 graphic file with name nihms373510t7.jpg 12.6 ± 1.1 84.9 ± 13.6
7 graphic file with name nihms373510t8.jpg 13.0 ± 1.1 28.1 ± 5.1
8 graphic file with name nihms373510t9.jpg 13.2 ± 1.0 68.1 ± 10.3
1 graphic file with name nihms373510t10.jpg 8.7 ± 0.6 11.3 ± 0.7
Amantadine graphic file with name nihms373510t11.jpg 15.7 ± 1.2 > 500

IC50 values were measured versus A/M2 from the Udorn strain of the virus, or the V27A mutant expressed in Xenopus laevis oocytes. All compounds were tested in hydrochloride salt form. The proton currents and extent of inhibition in the presence of various concentrations of drug were measured as described in methods.