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. 2022 Aug 16;37(1):2169–2178. doi: 10.1080/14756366.2022.2110089

Table 3.

Structures of (3-methoxybenzyl)thioureas (series C) and their rat TRPV1 agonist activities as log(1/EC50) (μM) values (reference25).

Inline graphic
  R1 R2 log(1/EC50)
C_1a H 4-Cl-benzyl 1.125
C_1b H 4-Cl-phenethyl 1.252
C_1c H (E)- 4-chlorostyryl 0.387
C_1d H (Z)- 4-chlorostyryl 1.387
C_1e H 4-F-phenethyl 0.886
C_1f H 2,4-dichlorophenethyl 0.886
C_1g H phenethyl 0.319
C_1h H 3-(4-chlorophenyl)propyl 0.319
C_1i H 4-(tert-butyl)benzyl 0.292
C_2a ‒(CH2)2-NH2 4-Cl-phenethyl 0.022
C_2b ‒(CH2)2-NH2 phenethyl −0.435
C_2c ‒(CH2)2-NH2 4-F-phenethyl −0.362
C_2d ‒(CH2)2-NH2 2,4-dichlorophenethyl 0.495
C_2e ‒(CH2)2-NH2 4-I-benzyl −0.127
C_2g ‒(CH2)2-NH2 4-(tert-butyl)phenyl −0.220
C_2h ‒(CH2)2-NH2 4-(tert-butyl)benzyl 0.770
C_2i ‒(CH2)2-NH2 3,5-di-tert-butylbenzyl 0.658
C_2j ‒(CH2)2-NH2 4-(tert-butyl)phenethyl 0.149
C_3 ‒(CH2)3-NH2 4-Cl-phenethyl −0.739
C_4 ‒(CH2)2-NH-CH3 4-Cl-phenethyl −0.847
C_5 ‒(CH2)2-N(CH3)2 4-Cl-phenethyl −0.547
C_8 ‒(CH2)2-NH-COCH3 4-Cl-phenethyl −0.710