. Author manuscript; available in PMC: 2023 Nov 23.

Published in final edited form as: Org Biomol Chem. 2022 Nov 23;20(45):8932–8943. doi: 10.1039/d2ob01545e

Table 4. Inhibition (IC₅₀, K_i ,in square brackets, and selectivity index SI^a,b) of class II GH38 α-mannosidases (GMIIb, AMAN-2, LManII and JBMan) by N-substituted 1,4-dideoxy-1,4-imino-D-lyxitol derivatives.

Compound	IC₅₀ [K_i](μM)				SI^a	SI^b
Compound	GMIIb	AMAN-2	LManII	JBMan	SI^a	SI^b
6	3.9 ± 0.1	2.3 ± 0.1	30.5 ± 3	10.5 ± 1.3	8	5
4	11.0 ± 1.3	8.7 ± 0.1	675 ± 67	1075 ±185	61	124
16	4.4 ± 0.2	3.5 ± 0.1	460 ± 53	940 ± 24	105	269
17	7.6 ± 1.1	2.4 ± 0.1	845 ±170	1950 ± 250	111	812
18	0.45 ± 0.08	0.21 ± 0.10	12.0 ± 1.3	18.0 ± 1.7	27	86
18	[0.16 ± 0.01]	[0.15 ± 0.03]	[3.9 ± 0.1]	[6.5 ± 0.5]	27	86
19	3.5 ±0.3	17.3 ± 0.1	190 ± 53	1290±113	54	75
20	15.5 ± 0.5	84.3 ± 0.1	980 ±102	2550±63	63	30
9	2.4 ± 0.1	12.5 ± 0.1	340 ± 35	115 ± 6.7	142	9
9	[0.83 ± 0.08]	[10.3 ± 1.0]	[165 ± 12.5]	[52.4 ± 7.5]	142	9
21	0.40 ± 0.05	2.3 ± 0.1	11.8 ± 1.2	20.3 ± 4.4	30	9
25	0.45 ± 0.10	2.7 ± 0.1	8.3 ± 2.1	8.3 ± 1.2	18	3
26	0.19 ± 0.02	1.4 ± 0.1	6.7 ± 1.2	4.7 ± 1.2	35	3
26	[0.04 ± 0.01]	[0.78 ± 0.23]	[3.2 ± 1.2]	[1.4 ± 0.4]	35	3
Swainsonine	0.0045	0.004 ± 0.02	0.012	0.20^d	3	20
Swainsonine	[0.0027]^e	0.01^c	[0.0071]^e		3	20
DIM^f	0.19 ± 0.04	0.81 ±0.03	2.55 ± 0.10	0.72 ± 0.03	13	1
DIM^f	[0.13 ± 0.02	[0.68 ± 0.03]	[1.95 ± 0.35]	[0.38 ± 0.03]	13	1

SI = [IC₅₀(LManII)/IC₅₀(GMIIb)]

SI = [IC₅₀(JBMan)/IC₅₀(AMAN-2)]

IC₅₀ estimated from inhibition assays measured by Paschinger et al.³⁴ where 45% inhibition of AMAN-2 by 10nM of swainsonine was found

IC₅₀ measuared by Poláková et al.³⁸

IC₅₀ and K_i measuared by Nemčovičová et al.²⁰

1,4-dideoxy-1,4-imino- D-mannitol

Table 4. Inhibition (IC50, Ki ,in square brackets, and selectivity index SIa,b) of class II GH38 α-mannosidases (GMIIb, AMAN-2, LManII and JBMan) by N-substituted 1,4-dideoxy-1,4-imino-D-lyxitol derivatives.