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A novel series of selective 1,2,4-triazole nonnucleoside reverse transcriptase inhibitors (NNRTIs) is described. In MT-4 cells compound, 4f inhibited human immunodeficiency virus type 1 (HIV-1) induced cytopathology at an IC50 of 9.98 μM with a selectivity index of 18.6. The hypothetical docking model of RT/4f derived from X-ray crystallographic structure of capravirine complex with HIV-1 RT links the activity profile to the H-bonding network.
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Lagoja et al. (2002) studied this question.
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