Table 2.

Activity of series 1 (compounds 1–26) against TryR.

Compd	R1	R2	R3	R4	TryR IC50 [μm]
1	CH2CH2NMe2	6-Br	5′-Methyl-furan-2-yl	H	1.7
2	CH2CH2NHMe	6-Br	5′-Methyl-furan-2-yl	H	1.1
3	CH2CH2NMe3+	6-Br	5′-Methyl-furan-2-yl	H	1.2
4	CH2CH2-N-morpholine	6-Br	5′-Methyl-furan-2-yl	H	4.2
5	2-pyridyl methyl	6-Br	5′-Methyl-furan-2-yl	H	4.7
6	3-pyridyl	6-Br	5′-Methyl-furan-2-yl	H	7.2
7	CH2CH2CH2-N-imidazole	6-Br	5′-Methyl-furan-2-yl	H	5.1
8	CH2CH2NMe2	6-Cl	5′-Methyl-furan-2-yl	H	3.1
9	CH2CH2NMe2	7-Br	5′-Methyl-furan-2-yl	H	5.7
10	CH2CH2NMe2	8-Br	5′-Methyl-furan-2-yl	H	5.8
11	2-pyridyl methyl	H	5′-Methyl-furan-2-yl	H	12.1
12	CH2CH2NMe2	H	5′-Methyl-furan-2-yl	H	14.4
13	CH2CH2NMe2	6-Cl	4′-Methylphenyl	CH3	26.5
14	CH2CH2-N-morpholine	H	5′-Methyl-furan-2-yl	H	100
15	CH2Ph	6-Br	5′-Methyl-furan-2-yl	H	>100
16	CH2CH2 CH2-N-morpholine	6-Cl	5′-Methyl-furan-2-yl	H	11.6
17	CH2CH2NMe2	6-Br	3′-Methoxyphenyl	H	>100
18	CH2CH2NMe2	6-Br	Phenyl	H	>100
19	CH2C6H4-p-SO2NH2	6-Br	5′-Methyl-furan-2-yl	H	8.4
20	CH2CH2NMe2	6-Br	Furan-2-yl	H	32.4
21	CH2CH2NMe2	6-Br	Pyrid-4-yl	H	96.3
22	CH2CH2NMe2	6-Br	5′-Methyl-thiophen-2-yl	H	>100
23	-N-morpholine	6-Br	5′-Methyl-furan-2-yl	H	>100
24	CH2-furan-2-yl	6-Br	5′-Methyl-furan-2-yl	H	>100
25	CH2CH2Ph	6-Br	5′-Methyl-furan-2-yl	H	>100
26	CH2CH2NMe2	6-F	5′-Methyl-furan-2-yl	H	>100