Table 5.

Chemical structures of the studied 2-aminothiazol-4(5H)-one derivatives possessing 11β-HSD1 inhibitory activity

Compound	R	R1	R2	% of 11β-HSD1 inhibition 10 µM [18–23]	log I11β‐HSD1
1a	CH2=CH-CH2-	H	H	0	0
1b		H	CH3	0	0
1c		H	C2H5	0	0
1d		H	n-C3H7	0	0
1e		H	CH(CH3)2	0	0
1f		CH3	CH3	0	0
1 g		H	C6H5	0	0
1 h		H	p-BrC6H4	13.46	1.16
1i		C5H10cycl		71.27	1.86
1j		C3H6cycl		38.03	1.59
2b	CH3-	H	CH3	0	0.00
2c		H	C2H5	0	0.00
2d		H	n-C3H7	0	0.00
2e		H	CH(CH3)2	21.13	1.34
2f		CH3	CH3	22.25	1.37
2 g		H	C6H5	0	0.00
2 h		H	p-BrC6H4	17.00	1.26
2i		C5H10cycl		48.00	1.69
2j		C3H6cycl		23.00	1.38
3b		H	CH3	0	0.00
3c		H	C2H5	0	0.00
3d		H	n-C3H7	0	0.00
3e		H	CH(CH3)2	18.86	1.30
3f		CH3	CH3	18.06	1.28
3 g		H	C6H5	0	0.00
3 h		H	p-BrC6H4	27.58	1.46
3i		C5H10cycl		54.53	1.74
3j		C3H6cycl		20.94	1.34
4b		H	CH3	16.29	1.24
4c		H	C2H5	20.11	1.32
4d		H	n-C3H7	29.17	1.48
4e		H	CH(CH3)2	44.27	1.66
4f		CH3	CH3	29.70	1.49
4 g		H	C6H5	26.85	1.44
4 h		H	p-BrC6H4	10.31	1.05
4i		C5H10cycl		82.54	1.92
4j		C3H6cycl		23.61	1.39
5a		H	H	22.27	1.37
5b		H	CH3	62.15	1.80
5c		H	C2H5	69.22	1.85
5d		H	n-C3H7	72.37	1.87
5e		H	CH(CH3)2	76.40	1.89
5f		CH3	CH3	65.99	1.83
5 g		H	C6H5	46.32	1.68
5 h		H	p-BrC6H4	15.30	1.21
5i		C5H10cycl		82.82	1.92
5j		C3H6cycl		74.13	1.88
6b		H	CH3	10.94	1.08
6c		H	C2H5	21.33	1.35
6d		H	n-C3H7	56.58	1.76
6e		H	CH(CH3)2	82.93	1.92
6f		CH3	CH3	53.17	1.73
6 g		H	C6H5	64.29	1.81
6 h		H	p-BrC6H4	86.96	1.94
6i		C5H10cycl		90.49	1.96
6j		C3H6cycl		71.25	1.86