Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole has anti-infection and anti-cancer effects[1][2][3].
Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4[1].
Novel inhibitor of ER-to-cytosol protein dislocation, exhibiting anti-dengue and anti-Zika virus activity
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum[1]. Halofantrine blocks HERG potassium channels[2].
HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants[1].
MurA-IN-2 (compound 37), a chloroacetamide fragment containing a primary aliphatic amine, is a potent MurA inhibitor with an IC50 value of 39 μM. MurA-IN-2 has antibacterial activity and inhibits the bacterial cell wall synthesis[1].
Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia[1].
SARS-CoV-2 nsp13-IN-5 (compound C6) is a potent SARS-CoV-2 nsp13 inhibitor with IC50 values of 50 and 55 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-5 can be used for researching anti-COVID-19[1].
LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC50s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively[1].
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3].
MMV665916, a quinazolinedione derivative, is an antimalarial agent. MMV665916 displays antiplasmodial activity against P. falciparum FcB1 strain with EC50 value of 0.4 µM and presents the high selectivity index (SI>250)[1].
Clidanac is a potent anti-inflammatory agent. Clidanac can uncouple the oxidative phosphorylation and can be used for the research of rheumatoid arthritis[1].
Oleana-2,12-dien-28-oic acid is an HBV-DNA inhibitor, HBsAg and HBeAg inhibitor. Oleana-2,12-dien-28-oic acid can be used in hepatitis B virus infection disease research[1].
Phosphodiesterase-IN-1 (Compound 7) is a phosphodiesterase (PDE) inhibitor with anti-Plasmodium activity. Phosphodiesterase-IN-1 has antiproliferative activity against P. falciparum (strain 3D7) with an IC50 value of 0.64 μM[1].
Mab Aspartate Decarboxylase-IN-1 is a potent aspartate decarboxylase (PanD) inhibitor with an IC50 value of 56.3 µM. Mab Aspartate Decarboxylase-IN-1 shows antibacterial activity[1].
N7-Methyl-guanosine-5'-triphosphate-5'-adenosine (m7GpppA) diammonium is a dinucleotide cap analog that can be used for in vitro RNA transcription[1].
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Sancycline (Bonomycin; 6-Demethyl-6-deoxytetracycline) hydrochloride is a semi-synthetic tetracycline antibiotic[1].
Apigravin is a potent antibacterial agent. Apigravin shows antibacterial activity against Bacillus subtilis with a MIC value of 61 μM[1].
Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability[1].
Anti-MRSA agent 1 (Compound 13d) is a wonderful MRSA (MIC = 0.5 μg/mL) inhibitor. Anti-MRSA agent 1 (Compound 13d) could effectually relieve the development of MRSA resistance[1].
NIOCH 14 is a antiviral agent and a pro-drug. NIOCH 14 has antiviral activity against orthopoxviruses. NIOCH 14 can significantly lower proportions of infected mice, and virus production levels in the lungs. NIOCH 14 can be used for researching anti-smallpox[1][2].
HBV-IN-7 is a potent HBV inhibitor with an EC50 of 7 nM (WO2021213445A1, compound 5)[1].
MGB-BP-3 is an antibiotic that has been shown to be active against a broad range of important multi-resistant Gram-positive pathogens.
Bruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity[1][2].
Mycophenolic acid sodium is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid sodium is an immunosuppressive agent. Antiangiogenic and antitumor effects[1][2].
Acyclovir, a molecule tailored to inactivate the thymidine kinase of the herpesvirus, is a guanosine analogue antiviral drug. It is a drug for HSV infection by GlaxoSmithKline.IC50 Value: 0.53-0.75 uM [3]Target: HSVin vitro: Acyclovir sensitivity was determined in a plaque-reduction assay in Vero cells. IC50 Values were consistently 2-3 fold lower in B2 compared with the H strain of Vero cells. HSV Type 2 strains were 2-10-fold less sensitive than Type 1 strains [2]. in vivo: two patients experienced a recurrence during treatment with oral acyclovir (200 mg 4 times daily) for up to 12 weeks, compared with nine during placebo treatment (P = 0.016). There was no difference between acyclovir and placebo in the time to the next recurrence following completion of treatment [3]. low-dose oral acyclovirmay be effective in the prevention of HSV infection during OKT3 treatment of seropositive patients. Continuation of acyclovir prophylaxis for two to four weeks following the conclusion of OKT3 therapy may prevent occurrence of delayed infections [4].Clinical trial: Acyclovir to Treat Patients Co-infected With HIV and Herpes Viruses in Uganda. Phage2
Emtricitabine triphosphate tetrasodium salt is the tetrasodium salt form of Emtricitabine triphosphate (HY-131596). However，Emtricitabine triphosphate ((-)-Emtricitabine triphosphate) is the phosphorylated anabolite of Emtricitabine (HY-17427)，a nucleoside reverse transcriptase inhibitor，targeting to HIV and HBV[1].