Table 1.

B-ring analogs of GSM 4.

Cmpd	B-ring	Aβ42 IC50a	clogPb	Kin. Aq. Sol.c
4		163 ± 10	3.88	ntd
22a		660 ± 131	3.74	ntd
22b		>1000	3.13	ntd
22c		171 ± 67	3.49	4.6
22d		60 ± 15	3.28	4.5*
22e		89 ± 38	2.66	<1.6
23		468 ± 165	3.25	ntd

^aIC₅₀ represents the concentration in nM of compound required for reducing Aβ42 levels by 50%. The IC₅₀ values are the mean ± standard deviation of at least 2 determinations.

^bCalculated partition coefficient of the simulated ratio of the compound’s concentration in octanol to the compound’s concentration in water using ChemAxon fragment based approach.

^cKinetic aqueous solubility measured at pH 7.4 by UV/Vis absorbance in PBS buffer (μM).

^dnt = not tested - compound did not meet minimum activity threshold.