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. Author manuscript; available in PMC: 2020 Apr 6.
Published in final edited form as: ChemMedChem. 2018 Sep 13;13(20):2208–2216. doi: 10.1002/cmdc.201800417

Table 5.

TLR signaling inhibition by C3 BSC pyrazoles with C5 carboxylic acid derivatives.

graphic file with name nihms-1016986-t0026.jpg
Cmpd R5 IC50 (μM)
TLR9 TLR7 TLR2 TLR4 Tox.
53 CO2Me 6.29 ± 0.19 16.9 ± 0.4 15.7 ± 0.5 > 50 30.8 ± 1.3
54 CO2H > 50 n.d. n.d. n.d. > 50
55 CONH2 3.43 ± 0.15 5.96 ± 0.74 27.8 ± 2.5 > 50 17.7 ± 7.7
56 CN 7.89 ± 0.36 > 50 > 50 > 50 33.5 ± 3.5
57 NH2 3.81 ± 0.30 5.93 ± 0.04 > 50 > 50 33.1 ± 3.5
58 NHCO2Me 3.46 ± 0.31 3.18 ± 0.21 > 50 > 50 25.7 ± 5.9
59 NHC(O)Me 3.38 ± 0.14 7.25 ± 0.21 > 50 17.4 ± 0.33 14.9 ± 2.4
60 NHC(O)Et 2.93 ± 0.84 7.92 ± 0.15 > 50 > 50 38.8 ± 4.5

n.d. = not determined