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. Author manuscript; available in PMC: 2017 Sep 15.
Published in final edited form as: Bioorg Med Chem Lett. 2016 Jul 30;26(18):4487–4491. doi: 10.1016/j.bmcl.2016.07.071

Table 3.

Structure and activities of analogs 9 a.

graphic file with name nihms808861u3.jpg
Compound Ar hM5 Percent inhibition
4 (VU0549108) 1,3,5-TriMe-1H-4-pyrazole 88% (hM5 IC50 = 6.18 μM)
9a 1-Me-1H-4-pyrazole 27%
9b 1,3-DiMe-1H-4-pyrazole Inactive
9c 1,5-DiMe-1H-4-pyrazole 83%
9d 3-Cl-4-F-phenyl 83%
9e 3,5-DiF-phenyl 62%
9f 3,4,5-TriF-phenyl 55%
9g 3,5-DiMe-4-isoxazole 40%
9h 1-Me-4-imidazole Inactive
a

Average of three determinations with hM5 cells with an EC80 of ACh as a single point % inhibition at 10 μM. If not IC50 reported, the IC50 was >10 μM.