Pyronaridine-d4 (tetraphosphate) is the deuterium labeled Pyronaridine tetraphosphate[1]. Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection[2][3].
Saccharin sodium is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium has bacteriostatic and microbiome-modulating properties[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].
Fosravuconazole is a prodrug of ravuconazole, with antifungal activity.
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives[1][2].
Influenza NP (147-155) is a Kd restricted epitope from influenza nucleoprotein[1].
Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice[1].
Enzaplatovir (BTA-585, BTA-C585) is an orally bioavailable RSV fusion protein inhibitor for the treatment of respiratory syncytial virus infections. RSV Infection Phase 2 Discontinued
Gallinamide A is a potent inhibitor of cathepsin L with an IC50 value of 17.6 pM.
Caspofungin is a potent antifungal agent. Caspofungin inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan[1][2].
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G[1].
Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist[1][2][3].
Ermanin is a flavonoid isolated from Tanacetum microphyllum. Ermanin potently inhibits iNOS, COX-2 activities, and inhibits platelet aggregation. Ermanin has anti-inflammatory, anti-tuberculous and anti-viral/bacterial properties[1][2].
Septamycin (A 28695A) is a metal complexing polyether antibiotic. Septamycin is produced by a strain of Streptomyces hygroscopicus NRRL 5678. Septamycin has anticoccidial activity[1][2].
Artemitin is a flavonol found in Laggera pterodonta (DC.) Benth., with antioxidative, anti-inflammatory, and antiviral activity[1].
Mosnodenvir (JNJ-1802) is a pan-serotype dengue antiviral agent with a high barrier to resistance, and is safe and well-tolerated. Mosnodenvir blocks the NS3-NS4B interaction within the viral replication complex. Mosnodenvir shows picomolar to low nanomolar in vitro antiviral activity in mice[1][2].
Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property. Target: Fumarate ReductaseTiabendazole serves to block angiogenesis in both frog embryos and human cells. It has also been shown to serve as a vascular disrupting agent to reduce newly established blood vessels. Tiabendazole has been shown to effectively do this in certain cancer cells. Thiabendazole works by inhibition of the mitochondrial, helminth-specific enzyme, fumarate reductase, with possible interaction with endogenous quinone [1].Thiabendazole inhibited B16F10 proliferation in vitro in a dose- and time-dependent manner with an IC50 of 532.4 +/- 32.6, 322.9 +/- 28.9, 238.5 +/- 19.8 microM at 24, 48, and 72 h, respectively. Moreover, thiabendazole inhibited the angiogenesis and the migration of B16F10 cells in vitro. Furthermore, thiabendazole restrained transcription and translation of the VEGF gene in B16F10 in vitro, and the apoptotic percentage of B16F10 cells was increased after exposure to thiabendazole [2].
Boscalid is an anti-fungal agent. Boscalid is a succinate dehydrogenase (SDH) inhibitor[1].
Thermopsine is a quinolizidine alkaloid isolated from the fruits and pods and stem bark of Sophora velutina subsp. Thermopsine has antibacterial activity[1].
18BIOder is a neuroprotective inhibitor of GSK-3β, highly selectively inhibiting HIV-1. It is the second generation derivative of 6BIO.
Streptolydigin (Portamycin) is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor with a Ki of 18 μM and a Kd of 15 μM. Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases[1][2][3]. Streptolydigin possess potent antibacterial activity, particularly against anaerobes and some Gram-positive aerobes[4].
1,4-Epidioxybisabola-2,10-dien-9-one is a 1,4-epidioxy-bisabola-2,12-diene derivate, which can be isolated from Curcuma longa L. 1,4-Epidioxybisabola-2,10-dien-9-one exhibits antiviral activity against influenza virus A/PR/8/34 (H1N1) in the MDCK cell line with an IC50 of 16.79 ± 4.03 μg/mL[1].
ATV006 is a potent, orally active antiviral agent and ester prodrugs of GS-441524. ATV006 inhibits the replication of SARS-CoV-2 and its variants. ATV006 can be used for SARS-CoV-2 research[1].
HR1 is a mastoid protease. HR1 can increase the permeability of human erythrocyte membrane. HR1 can induce cytoplasmic membrane permeation in bacteria and mast cells [1].
Tetramycin B (4-Hydroxytetramycin A) is a polyene macrolide antibiotic, an antifungal active compound isolated from Streptomyces hygrospinosus var. Beijingensis. The antifungal activity of Tetramycin B is higher than that of Tetramycin A, and the C-4 hydroxyl of Tetramycin B plays an important role in its biological activity[1].
RN-18 is a HIV-1 viral infectivity factor (HIV-1 Vif) inhibitor with an IC50 of 6 μM in nonpermissive H9 cells.