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. Author manuscript; available in PMC: 2008 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2007 Sep 8;17(22):6206–6211. doi: 10.1016/j.bmcl.2007.09.023

Table 2.

Biological activities obtained for compounds 22, 25–34. The compounds were assayed as described under Table 1. Compounds 25–27, 29 and 34 have a relatively low water solubility due to their high lipophilicity. This is reflected in this assay by a similar or reduced activity at 25 µM versus 2.5 µM. Concentration-dependent increase in activity however was observed in full concentration response curves, with maximal effects at 10 µM.

Cpd R 2.5 µM of Cpd, 1 µM of GABA 25 µM of Cpd, 1 µM of GABA 1 µM of GABA
Effect (%) ± sem Effect (%) ± sem pEC50 ± sem Emax (%) ± sem
22 graphic file with name nihms33112t1.jpg 80 ±1 93 ± 5 6.06 ± 0.05 83 ± 4
25 graphic file with name nihms33112t2.jpg 90 ± 1 80 ± 2 5.56 ± 0.13 132 ± 14
26 graphic file with name nihms33112t3.jpg 125 ± 4 141 ± 6 5.46 ± 0.10 185 ± 15
27 graphic file with name nihms33112t4.jpg 122 ± 3 110 ± 0 5.78 ± .03 183 ± 4
28 graphic file with name nihms33112t5.jpg 82 ± 5 52 ± 4 - -
29 graphic file with name nihms33112t6.jpg 128 ± 4 70 ± 4 5.78 ± 0.03 137 ± 3
30 graphic file with name nihms33112t7.jpg 28 ± 1 32 ± 2 - -
31 graphic file with name nihms33112t8.jpg 36 ± 2 69 ± 6 - -
32 graphic file with name nihms33112t9.jpg 29 ± 1 39 ± 2 - -
33 graphic file with name nihms33112t10.jpg 40 ± 3 21 ± 7 - -
34 graphic file with name nihms33112t11.jpg 58 ± 11 59 ± 4 - -