Table 1.

Chemical modification of methyl acarviosin. (a) α-Glucosidase inhibitory activity of several anhydro, deoxy, and O-methyl derivatives. (b) α-Glucosidase inhibitory activity of several 1,4-anhydro derivatives 116a–h.

(a)
Compd	Inhibitory activity
	(IC50, µM) α-Glucosidase (Baker’s yeast)
70	0.98
77	0.38
102a	1.25
b	0.75
104	1.45

(b)
Compd				Inhibitory activity
				(IC50, µM) α-Glucosidase (Baker’s yeast)
	X	Y	Z
116a	OH	H	OH	0.10
b	N3	H	OH	0.29
c	NH2	H	OH	2.2
d	NHAc	H	OH	33
e	F	H	OH	0.18
f	H	OH	OH	0.50
g	H	H	OH	0.032
h	H	H	H	0.030