Table 2 Antiretroviral activity of selected compounds against HIV-1 mutant strains.

From: Discovery of diarylpyrimidine derivatives bearing piperazine sulfonyl as potent HIV-1 nonnucleoside reverse transcriptase inhibitors

Compound

EC50 (μM)a

L100I

K103N

Y181C

Y188L

E138K

F227L/V106A

18a1

0.050 ± 0.0061

0.023 ± 0.0067

0.10 ± 0.018

>6.91

0.028 ± 0.0055

0.35 ± 0.069

18a2

0.056 ± 0.019

0.040 ± 0.0072

0.11 ± 0.029

>4.51

0.036 ± 0.0081

0.38 ± 0.12

18a3

0.080 ± 0.021

0.043 ± 0.0075

0.11 ± 0.0055

>3.71

0.044 ± 0.011

0.41 ± 0.087

18a4

0.080 ± 0.011

0.036 ± 0.0020

0.14 ± 0.027

>4.53

0.040 ± 0.0099

0.28 ± 0.10

18a5

0.084 ± 0.034

0.029 ± 0.0020

0.090 ± 0.011

>59.27

0.033 ± 0.0062

0.30 ± 0.061

18b1

0.0037 ± 0.00062

0.0017 ± 0.00032

0.0064 ± 0.00067

0.74 ± 0.21

0.0064 ± 0.00054

0.0099 ± 0.0016

18b2

0.0044 ± 0.0011

0.0035 ± 0.0012

0.0063 ± 0.00061

0.58 ± 0.12

0.0082 ± 0.00076

0.011 ± 0.0029

18b3

0.0068 ± 0.0014

0.0062 ± 0.0019

0.012 ± 0.0025

0.94 ± 0.22

0.019 ± 0.0077

0.028 ± 0.017

18b4

0.020 ± 0.0055

0.0061 ± 0.0021

0.036 ± 0.0087

>18.01

0.040 ± 0.0054

0.027 ± 0.012

18b5

0.0062 ± 0.0012

0.0055 ± 0.00043

0.016 ± 0.0050

0.50 ± 0.025

0.019 ± 0.0053

0.021 ± 0.019

18c1

0.015 ± 0.0068

0.0073 ± 0.0018

0.028 ± 0.0029

5.46 ± 4.50

0.032 ± 0.0049

0.019 ± 0.0068

BH-11c

0.014 ± 0.0053

0.0037 ± 0.0016

0.027 ± 0.0025

1.32 ± 0.22

0.0094 ± 0.0050

0.21 ± 0.095

NVP

2.23 ± 0.98

6.04 ± 2.66

7.40 ± 1.78

>15.02

0.22 ± 0.12

>15.02

ETR

0.012 ± 0.0051

0.0043 ± 0.0010

0.018 ± 0.0038

0.025 ± 0.0076

0.018 ± 0.0072

0.025 ± 0.0072

EFV

0.053 ± 0.028

0.12 ± 0.024

0.0063 ± 0.0020

0.25 ± 0.056

0.0065 ± 0.0017

0.26 ± 0.10

RPVb

0.0015 ± 0.00

0.0013 ± 0.00036

0.0047 ± 0.00048

0.079 ± 0.00077

0.0058 ± 0.00011

0.082 ± 0.021

  1. aEC50: concentration required to achieve 50% protection of MT-4 cell cultures against HIV-1-induced cytopathicity, as determined using the MTT method (mean ± SD, n ≥ 4).
  2. bUsed for comparison. The data were obtained from the same laboratory using the same method (Prof. Christophe Pannecouque, Rega Institute for Medical Research, KU Leuven, Belgium)4.
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