Peritassine A, an alkaloid that could be isolated from Tripterygium wilfordii Hook. f., possesses anti-HIV activity[1][2].
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function[1].
Pradimicin A (PRM-A) is a potent antifungal agent, with an MIC of 4 μg/mL against Candida rugosa. Pradimicin A has antiviral activities against CoV, HIV and other enveloped viruses. Pradimicin A shows aggregation property, and can recognize d-Man in the presence of Ca2+ ion[1][2].
HIV-1 integrase inhibitor ((Z)-4-(3-(azidomethyl)phenyl)-2-hydroxy-4-oxobut-2-enoic acid) is uesful for anti-HIV.
NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.
Delavirdine mesylate is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI) of HIV-1.
Azulene (Cyclopentacycloheptene) is as an isomer of naphthalene with high anti-HIV activity. Azulene, isolated from the distillation of chamomile oil, is a scaffold in medicinal chemistry[1][2][3].
Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is a autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
2F5 epitope, a peptide gp41 (659-671), comprises the entire epitope for one of the three known antibodies capable of neutralizing a broad spectrum of primary HIV-1 isolates and is the only such epitope that is sequential. 2F5 epitope is recognized by broadly neutralizing antibodies 2F5[1][2].
Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma[1][2][3][4][5].
Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Fipravirimat is a potent HIV-1 inhibitor. Fipravirimat has the potential for HIV and AIDS research[1].
DENV-IN-7, a flavone analog, is a dengue virus (DENV) inhibitor with an EC50 value of 70 nM. DENV-IN-7 has low toxicity against normal cell and anti-dengue activity[1].
HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
Adenallene, a nucleoside analogue, is an anti-HIV compound. Adenallene inhibits replication and cytopathic effect of HIV-1 and HIV-2[1].
Calceolarioside A is phenylethanoid glycoside with moderate binding affinity on HIV gp41[1].
HIV-1 inhibitor-31 (compound 4) is a potent HIV-1 inhibitor. HIV-1 inhibitor-31 can be used for researching AIDS[1].
Atevirdine is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Atevirdine inhibits non-nucleoside reverse transcriptase that leads to viral multiplication[1].
GS-9822 is a potent, non-catalytic site HIV integrase inhibitor with wild type EC50 of 3 nM.
Delavirdine(U 90152) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI).IC50 Value: 0.26 uM (Recombinant HIV-1 RT) [1]Target: HIV-1 reverse transcriptase; NNRTIin vitro: U-90152 [1-(5-methanesulfonamido-1H-indol-2-yl-carbonyl)-4-[3-(1-methyl eth yl-amino)pyridinyl]piperazine], which inhibited recombinant HIV-1 RT at a 50% inhibitory concentration (IC50) of 0.26 microM (compared with IC50s of > 440 microM for DNA polymerases alpha and delta). U-90152 blocked the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates, including variants that were highly resistant to 3'-azido-2',3'-dideoxythymidine (AZT) or 2',3'-dideoxyinosine, with a mean 50% effective dose of 0.066 +/- 0.137 microM. U-90152 had low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 microM. In experiments assessing inhibition of the spread of HIV-1IIIB in cell cultures, U-90152 was much more effective than AZT. When approximately 500 HIV-1IIIB-infected MT-4 cells were mixed 1:1,000 with uninfected cells, 3 microM AZT delayed the evidence of rapid viral growth for 7 days. In contrast, 3 microM U-90152 totally prevented the spread of HIV-1, and death and/or dilution of the original inoculum of infected cells prevented renewed viral growth after U-90152 was removed at day 24 [1]. Asdelavirdine concentration was increased from 0 to 100 microM, the K(M) for diclofenac metabolism rose from 4.5+/-0.5 to 21+/-6 microM, and V(max) declined from 4.2+/-0.1 to 0.54+/-0.08 nmol/min/mg of protein, characteristic of mixed-type inhibition [2].in vivo: The mean values (+/- standard deviations) for the maximum concentration in serum (C(max)) of ritonavir, the area under the concentration-time curve from 0 to 12 h (AUC(0-12)), and the minimum concentration in serum (C(min)) of ritonavir before the addition of delavirdine were 14.8 +/- 6.7 micro M, 94 +/- 36 micro M. h, and 3.6 +/- 2.1 micro M, respectively. These same parameters were increased to 24.6 +/- 13.9 micro M, 154 +/- 83 micro M. h, and 6.52 +/- 4.85 micro M, respectively, after the addition of delavirdine(P is <0.05 for all comparisons). Delavirdine pharmacokinetic parameters in the presence of ritonavir included a C(max) of 23 +/- 16 micro M, an AUC(0-8) of 114 +/- 75 micro M. h, and a C(min) of 9.1 +/- 7.5 micro M [3].Toxicity: Clinical trial: Quality of Life of HIV-infected Participants Switched to Raltegravir Versus Other Antiretroviral Regimens. Phase 4
2-Hydroxyacetophenone is a principal root volatile of the Carissa edulis[1]. 2-Hydroxyacetophenone shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 1.8 mM[2].
FGI-106 tetrahydrochloride is a potent and broad-spectrum inhibitor with inhibitory activity against multiple viruses. FGI-106 tetrahydrochloride is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 tetrahydrochloride also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively[1].
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].
GSK2838232 inhibit HIV reverse transcriptase activity across a broad panel of HIV-1 isolates, extracted from patent WO/2013090664A1, compound51.
CDK9-IN-30 is a CDK9 inhibitor that inhibits HIV-1 viral replication[1].
IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM[1].
Lefitolimod (MGN 1703) is a DNA-based TLR9 agonist and an immune surveillance reactivator. Lefitolimod induces HIV-specific immune responses and can be used for the research of cancer and HIV-1[1][4].
DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities. Sequence: Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH2.
DGKα-IN-8 (Example 51) is a DGKα inhibitor (IC50=22.491 nM; EC50=0.256 nM). DGKα-IN-8 can be used to study cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection[1].
Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model[1][2].