Table 1.

Activity of N1- and N2-substituted compounds against TbPTR1

Compd	R1 group	R2 group	TbPTR1 [μm][a]
2[b]	H	H	288
3[b]	Et	H	>200
4	C(=O)Ph	H	>60
5[b]	CH2CH2Ph	H	24
6	CH2Ph	H	16
7	CH2-(2-chlorobenzene)	H	10
8	CH2-(3-chlorobenzene)	H	7.5
9	CH2-(4-chlorobenzene)	H	5.4
10	CH2-(2,5-dichlorobenzene)	H	3.7
11[b]	CH2-(3,4-dichlorobenzene)	H	0.4
12	CH2-(3,5-dichlorobenzene)	H	8.8
13	CH2-(2-methylbenzene)	H	15
14	CH2-(2-fluorobenzene)	H	21
15	CH2-(4-methylbenzene)	H	15
16	CH2-(4-tert-butylbenzene)	H	4.2
17	CH2-(3-trifluoromethylbenzene)	H	6.3
18	CH2-(4-bromobenzene)	H	3.1
19	CH2-pyrid-2-yl	H	53
20	CH2-pyrid-3-yl	H	54
21	CH2-naphth-1-yl	H	6.1
22	CH2-naphth-2-yl	H	2.8
23	CH2-(3,4-dichlorobenzene)	C(=O)CH3	>60

^[a]Data for each compound was determined in duplicate. values were calculated using BatchKi software (BioKin); see Shanks et al. for more details.¹⁴

^[b]Data for these compounds have been reported previously.¹³