Table 4. Biological and Physicochemical Evaluation of 2-Aminothiazoles and 2-Aminooxazoles.

		kinetic solubility (μM)
compd	MIC (μM)	water	PBS pH 7.4	HLM t1/2 (min)d	HLM Cl′int (mL min–1 kg–1)e	mean GSH conjugate area	GSH conjugate area ratio (%)
1	27.5a	24 ± 2.7	7.5 ± 1.1	22.4 ± 1.6	27.9	303	10.4 ± 1.7
2	13a	20 ± 2.4	1.2 ± 0.2	14.5 ± 0.5	42.9	616	13.9 ± 0.2
3	1.5b	54.9 ± 15	27.7 ± 8	3.3 ± 0.3	188.8	34	3.7 ± 0.5
4	0.16b	2.9 ± 0.5	2.4 ± 0.5	16.1 ± 0.2	38.8	111	7.1 ± 0.9
30	12.3a	5.2 ± 0.6	5.9 ± 0.5	22.6 ± 1.2	27.6	2117	14.2 ± 5
31	>100a	0.7 ± 0.2	1.1 ± 0.3	20.9 ± 1.4	29.9	467	14.2 ± 1.5
34	2.3a	9.1 ± 2	6.8 ± 1.1	2.7 ± 0.8	226.1	120	15.8 ± 1.3
36	6.9c	24 ± 4	9.3 ± 1.2	15 ± 0.1	41.5	82	2.1 ± 0.9

^aMIC values determined by MABA are means of replicate experiments (SD < 15%).¹⁰

^bMIC determined by microdilution.⁷

^cMinimun Inhibitory Concentration, determined by REMA method.

^dMeasured in human liver microsomes and expressed in minutes.

^eIntrinsic clearance was calculated as (0.693/in vitro τ_1/2) × (mL of incubation/mg of microsomes) × (45 mg of microsomes/g of liver) × (20 g of liver/kg of body weight).