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. Author manuscript; available in PMC: 2010 Dec 10.
Published in final edited form as: J Med Chem. 2009 Dec 10;52(23):7689–7705. doi: 10.1021/jm900695w

Table 5.

Antiviral activity of macrocyclic inhibitors against multi-drug resistant clinical isolates in PHA-PBMs

Virus SQV IDV APV LPV DRV 14b 14c
HIV-1ERS104pre
(wild-type: X4)
0.008 ± 0.005 0.043 ± 0.004 0.030 ± 0.005 0.034 ± 0.002 0.003 ± 0.0002 0.007 ± 0.002 0.005 ± 0.003
HIV-1MDR/B (X4) 0.27 ± 0.073
(34)
>1
(>23)
>1
(>33)
>1
(>29)
0.019 ± 0.012
(6)
0.089 ± 0.016
(13)
0.037 ± 0.016
(7)
HIV-1MDR/C (X4) 0.032 ± 0.002
(11)
>1
(>23)
0.37 ± 0.011
(12)
>1
(>29)
0.008 ± 0.006
(3)
0.029 ± 0.001
(4)
0.044 ± 0.002
(9)
HIV-1MDR/G (X4) 0.030 ± 0.002
(4)
0.34 ± 0.14
(5)
0.43 ± 0.004
(14)
0.26 ± 0.04
(8)
0.023 ± 0.006
(5)
0.028 ± 0.004
(4)
0.057 ± 0.012
(11)
HIV-1MDR/TM (X4) 0.26 ± 0.04
(33)
>1
(>23)
0.32 ± 0.007
(11)
>1
(>29)
0.004 ± 0.001
(1)
0.072 ± 0.014
(10)
0.027 ± 0.001
(6)
HIV-1MDR/MM (R5) 0.19 ± 0.05
(24)
>1
(>23)
0.21 ± 0.222
(7)
>1
(>29)
0.011 ± 0.002
(4)
0.055 ± 0.025
(8)
0.033 ± 0.010
(7)
HIV-1MDR/JSL (R5) 0.30 ± 0.02
(37)
>1
(>23)
0.62 ± 0.02
(21)
>1
(>29)
0.027 ± 0.011
(9)
0.21 ± 0.032
(30)
0.073 ± 0.07
(15)