Table 2. Permeability Coefficient of N-sulfonylhydrazone Prototypes (1–4) and Quality Control Standards Determined by the PAMPA-BBB Assay.
compounds | literature permeability (10–6 cm/s)a | experimental permeability (10–6 cm/s) | classificationc | pKab |
---|---|---|---|---|
atenolol | 0.8 | 0.10 ± 0.21 | BBB– | |
caffeine | 1.3 | 0.77 ± 0.58 | BBB– | |
enoxacin | 0.9 | 0.57 ± 0.12 | BBB– | |
hydrocortisone | 1.9 | 1.26 ± 0.78 | BBB– | |
ofloxacin | 0.8 | 0.29 ± 0.43 | BBB– | |
testosterone | 17 | 19.9 ± 0.53 | BBB+ | |
verapamil | 16 | 16.3 ± 1.74 | BBB+ | |
LASSBio-1771 (1) | 0.43 ± 0.54 | BBB– | 6.35 | |
LASSBio-1772 (2) | 4.18 ± 0.03 | BBB+ | ND | |
LASSBio-1773 (3) | 0.45 ± 0.63 | BBB– | 6.35 | |
LASSBio-1774 (4) | 9.01 ± 0.09 | BBB+ | ND |