nnrti-resistant

Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.

HIV-1-IN-85 is an orally active HIV-1 inhibitor with an IC50 of 72 nM. It exhibits potent inhibitory activity against wild-type (WT) HIV-1 and single mutant strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs), such as L100I, K103N, Y181C, Y188L, and E138K. Additionally, it shows moderate inhibitory activity against double mutant strains (F227L+V106A, RES056). In ICR mice, HIV-1-IN-85 demonstrates good in vivo safety and is suitable for research on HIV-1 infection.

GSK 224876 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). It has activity against efavirenz-resistant strains in the treatment of treatment-naive HIV-1-infected subjects.

HIV-1 inhibitor-30 (compound 10i) is a potent inhibitor of HIV-1, specifically targeting the RT DNA polymerase enzyme, showing strong antiretroviral activity with an EC50 value of 40 nM and an IC50 value of 80 nM. Moreover, it demonstrates significant effectiveness against seven NNRTI-resistant strains of HIV-1 (RT-K103N; RT-Y181C; RT-K103N, Y181C; RT-L100I, K103N; RT-Y188L; RT-K103N, G190A; RT-K103N, V108I), with IC50 values from 0.04 to 1.42 μM. This compound holds potential for AIDS research [1].

HIV-1 inhibitor-13 is an orally active HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) with an IC50 value of 0.14 μM against HIV-1 RT. HIV-1 inhibitor-13 is active against HIV-1 resistant strains (EC50: 2.85-18.0 nM).

HIV-1 Inhibitor-57 (Compound 12g) is an antiviral agent that potently inhibits both wild-type and five common NNRTI-resistant strains of HIV-1, exhibiting EC50 values between 0.024 and 0.0010 μM. It achieves this efficacy by forming supplementary interactions with residues surrounding the binding site in the HIV-1 reverse transcriptase (RT) [1].

HIV-1 Inhibitor-58 (Compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain IIIB and NNRTI-resistant strains like K103N and E138K in MT-4 cells at an EC50 of less than 50 nM. Additionally, it inhibits CYP2C9 and CYP2C19 with IC50 values of 2.06 μM and 1.91 μM, respectively. This compound is utilized in HIV infection research [1].

RO-0335 is a potent diphenylether nonnucleoside reverse transcriptase inhibitor. RO-0335 inhibits Wt HIV-1 (IC50 = 1.1 nM) and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates.

Mer-NF5003E is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1 reverse transcriptase (RT) with an EC50 of 50 μM. It exhibits inhibitory effects on both wild-type HIV-1 and various NNRTI-resistant strains (e.g., K103N, Y181C). Mer-NF5003E holds potential for use in HIV infection research.