Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
HIV-1 inhibitor-36 (Compound 2) is a potent HIV-1. HIV-1 inhibitor-36 has the potential for further development as novel latency reversing agents[1].
Lamivudine is a nucleoside reverse transcriptase inhibitors?(NRTIs). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus.
Ulonivirine (MK-8507) is an orally active non-nucleoside reverse transcriptase inhibitor with high antiviral activity. Ulonivirine can be used for the research of HIV-1 infection[1].
HIV-1 inhibitor-9 is found to be potent inhibitor against the wild-type (WT) HIV-1 strain or multiple NNRTI-resistant strains at low nanomolar levels.
Pegaldesleukin is a conjugate of polyethylene glycol and interleukin-2 (PEG-IL2). Pegaldeslukin has antiviral activity and has potential applications in HIV, possibly delaying the progression of HIV infection by retaining the immune repertoire[1][2][3].
Hypoglaunine D is an analogue of Triptonine B and acts as an anti-HIV compound. Hypoglaunine D inhibits HIV replication in H9 lymphocytes with an EC50 value of 22 μg/ml[1].
Dolutegravir-d6 (S/GSK1349572-d6) is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2][3].
Atazanavir(BMS-232632) is an highly potent HIV-1 protease inhibitor.IC50 value:Target: HIV-1 protease inhibitorAtazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor. It has a pharmacokinetic profile that supports once-daily dosing and has demonstrated a unique resistance profile and superior virologic potency compared with other antiretrovirals in vitro. In subjects with HIV, atazanavir (400 mg once daily) produced rapid and sustained improvements in viral load and CD4 counts in both antiretroviral-naive as well as previously treated patients when used in combination with dual nucleoside reverse transcriptase inhibitor (NRTI) treatment [1].After intravenous (iv), oral (po) and intraportal (ip) administration of ATV at a dosage of 7 mg/kg, AUCs in HL rats were 12.41, 5.24 and 8.89 microg/mLh, respectively, and were significantly higher than those in control rats (4.09, 1.70 and 3.38 microg/mLh). Despite the decrease of distribution volume (Vd(ss)), the terminal half-life (t(1/2)) in HL tended to be shorter than in control, and hepatic distribution of ATV in HL rats was 4.8-fold increases. These results suggested that the uptake of ATV into liver might counteract the decrease of Vd(ss). On the other hand, there was no significant difference in bioavailability, and the lymphatic transport to AUC showed no statistical change. In conclusion, although the protein binding rate and AUC were significantly increased, the pharmacokinetics of ATV might be tolerated in HL [2].Clinical indications: HIV-1 infection Toxicity: torsades de pointes
Indinavir(MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated [1]. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom [2].
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
Stavudine is a nucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.Target: HIV RT; NRTIsStavudine is a dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV. Stavudine is an analog of thymidine. It is phosphorylated by cellular kinases into active triphosphate. Stavudine triphosphate inhibits the HIV reverse transcriptase by competing with natural substrate, thymidine triphosphate. It also causes termination of DNA synthesis by incorporating into it [1]. Mice were treated for 2 weeks with stavudine d4T (500 mg/kg/day), L-carnitine (200 mg/kg/day) or both drugs concomitantly. Body fatness was assessed by dual energy X-ray absorptiometry, and investigations were performed in plasma, liver, muscle and WAT. D4T reduced the gain of body adiposity, WAT leptin, whole body FAO and plasma ketone bodies, and increased liver triglycerides and plasma aminotransferases with mild ultrastructural abnormalities in hepatocytes [2].Clinical indications: HIV-1 infection FDA Approved Date: June 24, 1994 Toxicity: peripheral neuropathy; lipodystrophy
HBV Seq2 aa:179-186 serve as effective motifs for CTL response in H-2b system after in vitro restimulation of the primed T cells. HBV Seq2 aa:179-186 is a novel epitope identified on the surface antigen of hepatitis B virus[1].
Tenofovir diphosphate disodium is an antiretroviral agent and an inhibitor of DNA polymerases. Tenofovir diphosphate disodium is a substrate of HIV-1 reverse transcriptase (RT). Tenofovir diphosphate disodium can be used for the research of Aids[1].
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities[1].
Amylmetacresol is a local anesthetic and possesses antiviral (such HIV) effect. Amylmetacresol has the potential for the study in sore throat[1].
L-2'-Fd4C, is an l-nucleoside analogue. L-2'-Fd4C has anti-human immunodeficiency virus (HIV) and anti-hepatitis B virus (HBV) activity[1].
Raltegravir (potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.
3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
Feglymycin is a HIV replication inhibitor. Feglymycin is also an antibiotic peptide that has antibacterial activity (MIC: 32-64 μg/mL for Staphylococcus aureus)[1].
Vicriviroc maleate is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
2',3'-Dideoxyadenosine is an inhibitor of HIV replication[1]. Antiretroviral activity[1]. Antiviral efficacy[1].
HIV-IN-2 (Compound 100) is a potent inhibitor of HIV. HIV-IN-2 has the potential for the research of HIV infection[1].
Wilfortrine is a bioactive sesquiterpene alkaloid. Wilfortrine exhibits immunosuppresive effects. Wilfortrine also can inhibit leukaemia cell growth in mice and shows anti-HIV activity[1].
HIV-1 inhibitor-47 is an inhibitor of HIV-1, and inhibits vif-dependent degradation of human APOBEC3G, with an IC50 value of 14.33 μM. HIV-1 inhibitor-47 also involves in derivatives of 1-(2-pyrimidinyl)piperazine synthesis, with potential antianxiety, antidepressant, and antipsychotic effect[1][2][3].
F1839-I is a compound that can be isolated from Stachybotrys. F1839-I has weak cytotoxicity and anti-HIV activity with an IC50 value of 15.6 μM[1].
HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent[1].
NBD-556 is small molecule mimetic of CD4, NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.IC50 Value: Target: HIVNBD-556 N-phenyl-N′-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamide analogs as a novel class of human immunodeficiency virus type 1 (HIV-1) entry inhibitors that block the gp120–CD4 interaction. Human immunodeficiency virus (HIV-1) interaction with the primary receptor, CD4, induces conformational changes in the viral envelope glycoproteins that allow binding to the CCR5 second receptor and virus entry into the host cell. The small molecule NBD-556 mimics CD4 by binding the gp120 exterior envelope glycoprotein, moderately inhibiting virus entry into CD4-expressing target cells and enhancing CCR5 binding and virus entry into CCR5-expressing cells lacking CD4.
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure[1][2].
SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase[1]. SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism[2].