Table 5. UUI, MIA, and Pharmacokinetic Profiles of 1,2-Dihydro-3H-1,3-benzothiazole Derivatives.

Compound	R1	R2	UUIa IC50 (μM)	MIAb IC50 (μM) or %	Cmaxc (μg/mL)	Exc.d (%)
8	CN	CF3	>100	12%
9*	CN	CF3	13.1	55 μM	3.15	0.1
10	CN	Cl	>100	20%	1.35	23
11	Cl	Cl	6.8	27 μM	9.14	1.1
12	CN	iPr	83.3	12 μM	4.46	0.1
13	CN	Et	>100	37 μM	4.24	1.7
14	CN	ethynyl	3.2	13%	1.58	12.4
15	CN	SMe	7.1	21%	1.08	9.4
16	CF3	Cl	2.6	18 μM	6.41	0.1
17	F	Cl	33.9	63 μM	7.70	4.3
18	Cl	SMe	5.7	59 μM	4.64	0.2
19	CF3	OMe	17.8	47%	3.99	0
20	Cl	OMe	4.3	49%	1.06	0.1

^aUUI and

^bMIA are defined in Table 1.

^cC_max and

^dExc. are defined in Table 3.