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. Author manuscript; available in PMC: 2016 May 15.
Published in final edited form as: J Org Chem. 2015 Apr 30;80(10):4835–4850. doi: 10.1021/acs.joc.5b00550

Table 2.

In Vivo pharmakokinetic parameters of inhibitors in female Sprague-Dawley rats (n = 3, mean ± SD) following a single intravenous (i.v.) and oral (p.o.) administration

Compound i.v. PK parametersa
p.o. PK parametersb
AUC0-inf (μg.min.mL–1) CL (mL.min–1.kg–1) t1/2 (min) Cmax (μg.mL–1) AUC0-inf (μg.min.mL–1) F (%)
10c 519 ± 115 4.9 ± 0.9 11.2 ± 2.2 0.40 ± 0.20 66 ± 41 1.3 ± 0.7
11c 304 ± 60 8.4 ± 1.9 10.6 ± 0.7 0.70 ± 0.07 100 ± 14 3.5 ± 0.2
graphic file with name nihms-740683-t0023.jpg 1040 ± 330 2.5 ± 0.9 32.5 ± 7.4 0.46 ± 0.30 187 ± 11 1.8 ± 0.9
graphic file with name nihms-740683-t0024.jpg 913 ± 65 2.7 ± 0.2 31.7 ± 1.9 1.09 ± 0.03 422 ± 70 4.7 ± 1.1
graphic file with name nihms-740683-t0025.jpg 366 ± 33 6.9 ± 0.3 17.4 ± 1.4 0.64 ± 0.22 84 ± 12 2.3 ± 0.4
graphic file with name nihms-740683-t0026.jpg 807 ± 78 3.1 ± 0.3 37.0 ± 1.7 0.92 ± 0.04 266 ± 2 3.5 ± 0.2
graphic file with name nihms-740683-t0027.jpg 312 ± 54 8.5 ± 1.6 17.2 ± 1.3 0.97 ± 0.42 362 ± 85 11.4 ± 0.3
graphic file with name nihms-740683-t0028.jpg 10100 ± 2200 0.24 ± 0.06 267 ± 36 5.99 ± 0.56 4730 ± 540 5.3 ± 1.3
a

i.v. dose (Di.v.) = 2.5 mg/kg

b

p.o. dose (Dp.o.) = 25 mg/kg

c

reference 34.

AUC0-inf: area under the plasma concentration-time curve from time 0 to infinity, CL: clearance, t1/2: terminal elimination half-life, Cmax: maximum plasma concentration, F: relative oral bioavailability calculated as follows F = 100 × [(AUCp.o. × Di.v.)/(AUCi.v. × Dp.o.)].