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. Author manuscript; available in PMC: 2020 Oct 16.
Published in final edited form as: Bioorg Med Chem. 2010 May 25;18(14):5208–5223. doi: 10.1016/j.bmc.2010.05.057

Table 4.

Effect of the 9-N-substituent with heteroaryl moieties on activity profiles

graphic file with name nihms-1634538-t0045.jpg
Compds R C3 Configuration (3R and/or 3S) IC50 (nM) Ca assay Stability in rat liver microsomesa remaining% cLog Pb
23 graphic file with name nihms-1634538-t0046.jpg (3RS) 21 10 6.16
24 graphic file with name nihms-1634538-t0047.jpg (3S) 71 29 6.16
25 graphic file with name nihms-1634538-t0048.jpg (3RS) 35 23 6.05
26 graphic file with name nihms-1634538-t0049.jpg (3RS) 160 NTc 5.49
27 graphic file with name nihms-1634538-t0050.jpg (3S) 450 NTc 5.55
28 graphic file with name nihms-1634538-t0051.jpg (3RS) 570 NTc 6.00
1a graphic file with name nihms-1634538-t0052.jpg (3RS) 28 33 7.66
a

The data show the remaining% 15 min after incubating with the 0.5 mg/mL rat liver microsomes.

b

Calculated by ADMET predictor (ver. 4.0).

c

NT: not tested.