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. 2011 Aug 29;2(11):840–844. doi: 10.1021/ml2001517

Table 2. SAR for Lactic Acid Ethers (Series 2).

graphic file with name ml-2011-001517_0003.jpg

					mouse microsomes		human microsomes
compd no.	R^a	MWt^b	clog P^b CHI^b	Pf^b IC₅₀ (μM)	CLi^c (mL/min/g)	t_1/2 (min)	CLi^c (mL/min/g)	t_1/2 (min)
15	H	376.3	3.44	0.897	5.3	12.0	2.9	24.7
15	H	376.3	3.52	0.897	5.3	12.0	2.9	24.7
16	2-Cl	410.8	4.06	0.190	5.6	11.7	1.6	>30
16	2-Cl	410.8	3.71	0.190	5.6	11.7	1.6	>30
17	3-Cl	410.8	4.29	0.327	7.9	6.2	1.2	>30
17	3-Cl	410.8	3.84	0.327	7.9	6.2	1.2	>30
12	4-Cl	410.8	4.29	0.394	4.1	13.6	3.3	21.8
12	4-Cl	410.8	3.84	0.394	4.1	13.6	3.3	21.8
18	3-CF₃	444.3	4.57	0.285

^a

All compounds racemic where applicable.

^b

See Table 1 for abbreviations.

^c

In vitro intrinsic clearance.