| Cpds |
R |
MW |
OBAV, % |
cLogPb |
| 2.8 |
H |
354.7 |
1 |
-0.73 |
| 4.1 |
-(CH2)2COPh |
683.2 |
0 |
8.06 |
| 4.2 |
-CH2Ph-(3-Cl-4-OAc) |
663.9 |
0 |
7.89 |
| 4.3 |
-CH2Ph-(3,4-di-OAc) |
767.1 |
1 |
3.61 |
| 4.4 |
-CH2Ph-(3-Me-4-OAc) |
679.1 |
1 |
6.56 |
| 4.5 |
-CH2Ph-(3-OMe-4-OAc) |
711.1 |
1 |
5.29 |
| 4.6 |
-CH2Ph-(3-Br-4-OMe) |
752.8 |
1 |
7.94 |
| 4.7 |
-CH2OCOOPh-(2-Me) |
683.0 |
1 |
7.17 |
| 4.8 |
-CH2OCOBu-t |
583.0 |
0 |
6.07 |
| 4.9 |
-CH2OCOPr-i |
555.0 |
1 |
5.37 |
| 4.10 |
-CH2OCOPh |
623.0 |
1 |
7.65 |
| 4.11 |
-CH2SCOPh |
655.1 |
1 |
7.73 |
| 4.12 |
-CH2OCOPh-(4-F) |
659.0 |
0 |
7.82 |
| 4.13 |
-CH2OCO(3-furyl) |
602.9 |
1 |
5.81 |
| 4.14 |
-CH2OCO(2-furyl) |
602.9 |
1 |
5.24 |
| 4.15 |
-CH2OCO(2-thienyl) |
635.0 |
1 |
6.86 |
| 4.16 |
-CH2OCO[3-pyridyl-(6-Cl)] |
693.9 |
1 |
6.31 |
| 4.17 |
-CH2OCO[3-pyridyl-(6-Br)] |
782.8 |
0 |
6.59 |
aOBAV determined by measuring urinary excretion of 2.8 following oral
administration of the prodrug vs i.v. administration of 2.8; bADME Boxes version
3.5 (Pharma Algorithm, Toronto, Canada) was used |
