hiv-1 infection

The N-dealkylated metabolite (M1) of Atazanavir, a HIV protease inhibitor.

PSB-0739 Selective platelet P2Y12 receptor antagonist characterized by competitive binding and high affinity (Ki =24.9 nM) with antithrombotic and platelet aggregation modulating effects.

Q-VD-OPh is an irreversible caspase inhibitor with an IC50 value of 48 nM against caspase-7 and between 25 and 400 nM against caspase-1, 3, 8, 9, 10, 12. Q-VD-OPh inhibits HIV infection and can cross the blood-brain barrier.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

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.

Opaviraline (GW-420867X) is a potent reverse transcriptase inhibitor that inhibits Human immunodeficiency virus 1 and has the potential to treat HIV infection.

KM-023 is a new second-generation non-nucleoside reverse transcriptase inhibitor for the study of human immunodeficiency virus (HIV) type 1 infection.

Dolutegravir intermediate-1 (1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid) is a new synthetic Dolutegravir intermediate. Dolutegravir is an integrase inhibitor developed for the treatment of human immunodeficiency virus (HIV)-1 infection.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

PF-3450074 (PF-74) acts at an early stage of HIV-1 infection inhibits viral replication by directly competing with the binding of CPSF6 (nuclear host factors cleavage and polyadenylation specific factor 6) and NUP153 (nucleoporin 153), and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. PF-3450074 is a specifical inhibitor of HIV-1 capsid protein (CA) and shows a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM).

Fostemsavir Tris (BMS-663068 Tris) is the prodrug of BMS-626529,is a oral, safe and effective inhibitor of HIV-1 attachment. It inhibits human immunodeficiency virus type 1 (HIV-1) infection by binding to gp120 and interfering with the attachment of virus to CD4+ T-cells.

Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]

HIV-1 inhibitor-3 is an HIV infection inhibitor.

AZT-PMPA, an aryl phosphate derivative of AZT and a nucleoside analogue, demonstrates anti-HIV activity[1]. As a nucleoside reverse transcriptase inhibitor (NRTI), AZT-PMPA targets HIV infection effectively[2].

Elsulfavirine (VM-1500) is an HIV-1 infection reverse transcriptase inhibitor. It is a new anti-HIV drug.

Gardiquimod is a TLR7/8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

HIV-1 integrase inhibitor 2 is used for the treatment of human immunodeficiency virus (HIV) infection.

Gardiquimod (hydrochloride) is an imidazoquinoline class TLR7/8 agonist. It can inhibit HIV-1 infection in macrophages and activated peripheral blood mononuclear cells (PBMCs). At concentrations below 10 μM, Gardiquimod (hydrochloride) specifically activates TLR7.

NPD4456 (Compound 3) is a 3-phenylcoumarin Vpr inhibitor. It binds competitively to Vpr and inhibits HIV-1 virus infection.

HIV-1inhibitor-82 (Compound L14) is a small molecule inhibitor of HIV-1 entry with oral bioavailability, exhibiting an IC50 value of 0.39 μM. It holds potential for research in combating HIV-1 infection.

HIVCapsid-IN-2 (Compound IC-2b4) is a potent inhibitor of the HIV-1 capsid protein (CA). It effectively inhibits both HIV-1, with an EC50 of 0.08 μM, and HIV-2. HIVCapsid-IN-2 operates by directly stabilizing the binding to HIV-1 CA, exerting its inhibitory effects in both early and late stages of infection.

FC-14367 is a PROTAC degrader targeting the HIV-1Nef protein. It forms a ternary complex by binding Nef with CereblonE3 ubiquitin ligase, inducing ubiquitination of Nef and its subsequent proteasomal degradation. This restores cell surface CD4 and MHC-I expression, inhibiting HIV-1 replication. FC-14367 is useful for research on HIV infection and AIDS.

ATPase-IN-6 is an inhibitor of H+/K+-ATPase (ATPase) and a derivative of imidazopyridine. It exhibits significant antiviral activity against various viruses, such as HIV-1 and SARS-CoV-2. ATPase-IN-6 is applicable in antiviral infection research.

FC-14369 is a PROTAC degrader targeting the HIV-1Nef protein (HIV-1Nef protein) with a DC50 value of 160 nM. By means of its bifunctional structure, FC-14369 binds to both Nef and Cereblon E3 ubiquitin ligase, facilitating Nef ubiquitination and proteasomal degradation. This action restores the expression of cell surface CD4 and MHC-I, thereby inhibiting HIV-1 replication. FC-14369 is applicable in the study of HIV infection and AIDS.