reverse transcriptase-in-1

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

Punicalin exerts anti-inflammatory, antioxidative, and anti-hepatotoxic activities, it shows inhibitory activity on HIV-1 reverse transcriptase in a dose-dependent manner, with an IC50 of 0.11 microg/ml (0.14 microM).

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

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.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Nevirapine (NVP) is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

Bavtavirine is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) that inhibits HIV replication by inhibiting HIV-1 reverse transcriptase activity and preventing the transcription of viral RNA into DNA for use in Highly Active Antiretroviral Therapy (HAART) programs and HIV disease studies

beta-L-D4A, a nucleoside HIV-1 reverse transcriptase inhibitor, exhibits biological activity by terminating DNA chain synthesis in the 5'-3' direction.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

Loviride is a non-nucleoside reverse transcriptase inhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reverse transcriptase from HIV-1.

HIV-1inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor with an EC50 range of 0.0039-0.338 μM. Its target is the reverse transcriptase, exhibiting an IC50 value of 0.055 μM. Additionally, HIV-1inhibitor-75 demonstrates good metabolic stability in vitro, presenting moderate clearance rates and an extended half-life in human plasma and liver microsomes.

HIV-1inhibitor-76 (compound 9t-2) is an inhibitor of the HIV-1 non-nucleoside reverse transcriptase. It is utilized in research aimed at combating HIV.

TAC (TERT activator compound) is a TERT (telomerase reverse transcriptase) activator that enhances TERT transcriptional activity through the MEK/ERK/AP-1 cascade pathway, promotes telomere synthesis in primary human cells and naturally aged mice, reduces cellular senescence and inflammatory cytokines, and alleviates neuroinflammation, among other effects.

NRTT-IN-1 (Compound 1) is an inhibitor of the nucleoside reverse transcriptase translocation (NRTT), effectively blocking HIV DNA synthesis and viral replication.

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.

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.

(+)-Carbovir triphosphate, an active metabolite of Abacavir, was utilized to study the molecular mechanism of inhibition and drug resistance in HIV-1 reverse transcriptase.

Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reverse transcriptase inhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re

AIC-292 is a potent reverse transcriptase inhibitor with well tolerated in different cell lines. In addition, activity of AIC292 could be demonstrated against a broad panel of wild-type HIV-1 group. AIC292 also retained activity against viruses harboring

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.

L-696229 is a specific inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). L-696229 inhibited RT activity in a mutually exclusive manner with respect to either phosphonoformate or azidothymidine triphosphate and was a weak

R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold

SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.