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. 2019 Nov 27;9:17640. doi: 10.1038/s41598-019-54158-2

Table 2.

Structure-activity data of selected pyrazoloquinoline analogs.

graphic file with name 41598_2019_54158_Figf_HTML.gif
Compound R1 R2 R3 EC50 (μM) Relative Vmax (%)*
D001 OMe H 2-chlorobenzene 15 90
D003 OMe H 4-pyridine >30 1
D010 OMe H 4-fluorobenzene 3.6 24
D012 OMe H 3,4,5-trimethoxybenzene >30 3
D018 OMe H 2-chloro-4-fluoro-benzene 2.4 92
D025 OMe H 3-methyl-4-nitro-benzene >30 3
D035 OMe H graphic file with name 41598_2019_54158_Figg_HTML.gif >30 1
D036 OMe H 3-nitro-4-chloro-benzene >30 11
D038 OMe H 2-chloro-4-nitro-benzene 1.7 100
D086 OMe H graphic file with name 41598_2019_54158_Figh_HTML.gif >30 3
D123 OMe H graphic file with name 41598_2019_54158_Figi_HTML.gif 0.3 100
D136 Me H 4-fluorobenzene 18 11
D138 H OMe 2-chloro-4-nitro-benzene 3.4 21

*100% Vmax corresponds to 20 μM ASP-11.