Table 1.

Molecular structures and PDE2A inhibitory activity of 11 representative benzo[1,4]diazepin-2-one derivatives examined in this study

Compound	R1	R2	R3	R4	IC50 (μM)
1	CH3	OCH3	(2,6-DiMeO)Ph	4-OCH3	0.0060
2	CH3	H	(2,6-DiMeO)Ph	4-OCH3	0.017
3	CH3	OCH3	(2,6-DiMeO)Ph	3-CONH2	0.020
4	CH3	H	(2,6-DiMeO)Ph	3-CONH2	0.030
5	CH3	OCH3	Ph	3-CONH2	0.050
6	CH3	OCH3	4-ClPh	3-CONH2	0.12
7	CH3	OCH3	Ph	3-CH2OCH3	0.30
8	CH3	H	(2,6-DiMeO)Ph	3-CH3	0.50
9	CH3	H	(2,6-DiMeO)Ph	3-CN	0.60
10	CH3	H	Ph	3-CONH2	1.1
11	CH3	H	Ph	3-CN	2.2