Table 2.

Drug-like properties in vitro of DAAN compounds

#	R1	aq. sol. (μg/mL)a		Log Pb	t1/2c
		pH 2.0	pH 7.4		HLM (min)	S9 (min)	human plasma (h)
8a	-CO2(CH2)2OCH3	1.64	0.77	>5	19	9.5	62
8b	-CO2(CH2)2CN	0.94	0.36	>5	17	12	32
8c	-CONH(CH2)2Cl	9.53	1.59	>5	61	74	8
8d	-CONH(CH2)3OH	19.9	1.01	3.22	ND	ND	ND
8e	-CON(CH2)2	94.2	1.20	2.21	158	110	12
8f	-CON(CH2)2CF2	57.6	6.59	3.58	14	14	57
8g	-CONHNH2	89.6	2.40	2.31	36	39	8
3	-CONH2	2.09	0.63	3.53	90	108	65
4a	-CONHMe	44.7	8.28	2.65	112	96	72
4b	-CONHEt	69.4	1.08	3.63	139	61	91
4c	-COOMe	21.8	1.21	4.15	18.5	7.7	89
2d		86.8	0.24	>5	108	102	92
propranolold					139	116	80

^aGeneral solubility guidelines for human oral absorption are < 10 μg/mL, low; 10–60 μg/mL, moderate; > 60 μg/mL, high.

^bMeasured in octanol-water at pH 7.4.

^cMetabolic stability incubation assay data from at least two experiments in parallel.

^dReference compound.