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. Author manuscript; available in PMC: 2018 Jun 1.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Apr 4;27(11):2479–2483. doi: 10.1016/j.bmcl.2017.04.009

Table 1.

Structures and mAChR activities of analogs 5, 14a–o.

graphic file with name nihms869431u3.jpg
Compound R hM4 IC50 (μM)a [% ACh Min ±SEM] hM4 pIC50 (±SEM)a
5 4-Et 0.38 [5.3±0.7] 6.46±0.09
14a H 0.65 [2.7±0.3] 6.21±0.09
14b 4-Me 0.31 [3.3±0.2] 6.52±0.08
14c 2-naphthyl 0.71 [6.8±2.2] 6.16±0.06
14d 3,4-methylenedioxy 0.51 [4.1±0.3] 6.30±0.09
14e 4-F 0.24 [3.5±0.2] 6.64±0.02
14f 3-F 0.31 [3.2±0.3] 6.52±0.06
14g 2-F 0.13 [3.2±0.5] 6.91±0.08
14h 4-Cl 0.14 [3.0±0.2] 6.88±0.07
14i 4-OMe 0.46 [5.3±1.0] 6.30±0.06
14j 2,3-diF 0.19 [3.1±0.1] 6.77±0.15
14k 2,4-diF 0.10 7.00±0.08
14l 2,5-diF 0.08 [3.1±0.2] 7.11±0.11
14m 2,6-diF 2.72 [7.0±0.9] 5.57±0.05
14n 2-F, 4-Cl 0.15 [3.1±0.3] 6.93±0.06
14o 2,4-diCl 0.27 [3.0±0.1] 6.58±0.09
a

Mean of three independent determinations in a calcium mobilization assay using recombinant hM4-expressing Chinese hamster ovary cells co-transfected with chimeric Gqi5 in the presence of an ACh EC80.