nnrti

Rilpivirine (R278474) is a diarylpyrimidine derivative and reverse transcriptase inhibitor with antiviral activity against HIV-1 that is used in the treatment of HIV infections.

Delavirdine mesylate (BHAP-U 90152 (mesylate)) is a non-nucleoside reverse transcriptase inhibitor (NNRTI).

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

NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with notable anti-resistance efficacy, effectively inhibiting both the wild-type HIV-1 and five mutant strains at EC50 values within the nanomolar range. This compound also exhibits favorable pharmacokinetic properties [1].

NNRTIs-IN-3 (compound 8) is an HIV-1 non-nucleoside reverse transcriptase inhibitor, displaying potent efficacy with an EC50 value of 0.01 µM [1].

NNRT-IN-10 is a potent, selective, and orally bioavailable non-nucleoside reverse transcriptase inhibitor (NNRTI) for HIV-1. The compound exhibits EC50 values ranging from 1.16 to 18.3 nM against HIV and its variants. NNRT-IN-10 has favorable pharmacokinetic properties and safety profile, making it suitable for research on AIDS caused by HIV-1.

NNRT-IN-2 (compound 7w) is an orally administered non-nucleoside reverse transcriptase inhibitor (NNRTI) that effectively suppresses both wild-type HIV-1 and various mutant strains. It inhibits HIV-1 reverse transcriptase with an EC 50 value of 22 nM. Additionally, NNRT-IN-2 exhibits insensitivity to CYP and hERG, demonstrating favorable safety and pharmacokinetic profiles [1].

NNRT-IN-5 (compound 10d) is an orally available non-nucleoside reverse transcriptase (Reverse Transcriptase) inhibitor.

NNRT-IN-6 (Compound 13a) is a non-nucleoside reverse transcriptase inhibitor (NNRT) used to inhibit HIV-1 reverse transcriptase (HIV-1RT), with an IC50 of 0.41 μM. It effectively suppresses both wild-type HIV-1 and mutants L100I, K103N, Y181C, Y188L, E138K, F227L/V106A, and RES056, with an EC50 range of 6.2-250 nM.

NNRT-IN-4 (Compound 10p) is an inhibitor of non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1RT. It exhibits antiviral activity against both wild-type and mutant strains of HIV-1, with an EC50 ranging from 6 to 63 nM. NNRT-IN-4 shows weak inhibitory activity on hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). In mice, NNRT-IN-4 demonstrates good tolerance and safety at 2 g/kg.

NNRT-IN-8 (compound 9K) is a potent non-nucleoside reverse transcriptase inhibitor, exhibiting EC50 values of 0.0014, 0.0041, and 0.0077 µM against HIV-1WT, K103N, and E138K, respectively.

NNRT-IN-9 (Compound EG28) is a non-nucleoside reverse transcriptase inhibitor (NNRT). It demonstrates strong antiviral and resistance-fighting activity against wild-type (WT) and various clinically relevant mutant strains (E138K and K103N + Y181C) of HIV-1, with EC50 values of 55 nM, 67 nM, and 3910 nM, respectively. NNRT-IN-9 is applicable in acquired immunodeficiency syndrome (AIDS) research.

NNRT-IN-11 (14l) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor, exhibiting EC50 values ranging from 6.50 to 52.9 nM against both wild-type (WT) and a range of HIV-1 mutant strains. NNRT-IN-11 demonstrates antiviral properties.

NNRT-IN-12 (compound 19) is a potent inhibitor of non-nucleoside reverse transcriptase (NNRT), exhibiting an IC50 value of 0.107 μM against WTHIV-1RT. It shows anti-HIV-1 activity with EC50 values of 14.1 nM, 5.03 nM, 7.64 nM, and 27.1 nM against the L100I, K103N, Y181C, and Y188L mutant strains of HIV-1, respectively. Additionally, NNRT-IN-12 demonstrates cytotoxicity.

NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly suppresses HIV-1 reverse transcriptase with an IC₅₀ of 0.25 μM. It exhibits excellent antiviral activity against wild-type HIV-1 (EC₅₀= 0.0046 μM) and various resistant mutants. NNRT-IN-13 also demonstrates favorable in vivo metabolism and safety, making it useful for HIV-related research.

NNRT-IN-15 (Compound 16 a) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor. It exhibits an EC50 of 3 nM against wild-type HIV-1 and effectively inhibits seven mutant strains (L100I, K103N, Y181C, etc.) with EC50 values ranging from 8.2 to 43.4 nM. The compound shows low cytotoxicity in MT-4 cells (CC50 = 196.46 μM) and also inhibits wild-type HIV-1RT and hERG channels with IC50 values of 0.7599 μM and 27.455 μM, respectively. NNRT-IN-15 is suitable for HIV-1 infection research.

IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.

UC-781 (NSC-675186) is a potent and selective inhibitor of human immunodeficiency virus HIV-1 non-nucleoside reverse transcriptase (NNRTI) I with a C50 value of 5 nM.UC-781 exhibits both antiviral activity and drug resistance.UC-781 is in a stable state, and is unaffected by lower pH or varying temperatures.

Fosdevirine (GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological related disorders such as late-onset epilepsy.

(Iso)-Fosdevirine ( (Iso)-GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological disorders such as late-onset epilepsy.

Etravirine (T2551) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. Etravirine-D4 is the deuterium labeled Etravirine.

ZK-316 is a potent and broad-spectrum NNRTI inhibitor with an EC50 range of 0.99 to 75.1 nM. It is applicable for HIV research.

HIV-1inhibitor-66 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits inhibitory activity against wild-type HIV-1 reverse transcriptase (HIV-1 reverse transcriptase) with an IC50 of 40 nM.

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.