Iseganan is an antimicrobial peptide, shows broad-spectrum anti-bacteria and fungi activity. Iseganan can be used in oral mucositis research[1][2][3].
RSV L-protein-IN-2 (Compound A) is a noncompetitive RSV polymerase inhibitor (IC50: 4.5 μM). RSV L-protein-IN-2 shows antiviral activity against long RSV strains (EC50: 1.3 μM)[1].
Tolytoxin, a bioactive metabolite from cyanobacteria, is a potent antifungal antibiotic, exhibiting MICs of 0.25-8 nmol. Tolytoxin is a cyanobacterial macrolide that targets actin by inhibition of its polymerization. Tolytoxin has cytotoxic effects in cancer cells[1].
GSK2200150A, identified by high-throughput screening (HTS) campaign, is an anti-tuberculosis (TB) agent.
Plumieride is an antifungal agent. Plumieride has strong fungitoxicity against some dermatophytes. Plumieride has little cytotoxic activity against the P388 leukaemia cell line with an IC50 of 85 μg/mL[1].
DNA Gyrase-IN-2 (Compound 22a) is a bacterial DNA gyrase B inhibitor with IC50s of 3.29-10.49 and 4.41-5.61 µM for E. coli DNA gyrase and M. tuberculosis DNA gyrase. Anti-tubercular and antibacterial activity[1].
Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials.Zabofloxacin hydrochloride (DW-224a) has excellent activity against gram-positive pathogens including Steptococcus aureus (S. aureus), Streptococcus pyogenes (S. pyrigenes), and S. pneumonia.Zabofloxacin hydrochloride (DW-224a) is considered as an alternative candidate for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP)[1].
Dermaseptin-B3 inhibits the growth of Gram-positive and Gram-negative bacteria (MIC: 1.3, 2.3, 5.0, 2.6, 2.3 μM for S. aureus, P. aeruginosa, P. aeruginosa, E. (ATCC 25922), E. (54127) respectively). Dermaseptin-B3 also inhibits tumor cell proliferation[1][2].
Acridone is an organic compound based on the acridine skeleton. Acridone has antibacterial, antimalarial, antiviral and anti neoplastic activities[1].
Amikacin hydrate (BAY 41-6551 hydrate), a semisynthetic analog of kanamycin, is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin hydrate (BAY 41-6551 hydrate) is ototoxic and nephrotoxic[1][2].
HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM[1].
RSV/IAV-IN-3 (compound 14'i) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza A virus (IAV) with EC50 values of 2.92 µM and 1.90 µM,respectively. RSV/IAV-IN-3 has antiviral effect against H1N1 and H3N2 with EC50 values of 3.25 µM and 1.50 µM in MDCK cells, respectively. RSV/IAV-IN-3 significantly inhibits the activity of luciferase in a dose-dependent manner, with an EC50 of 3.89 µM. RSV/IAV-IN-3 inhibits IAV infectivity and RdRp activity. RSV/IAV-IN-3 inhibits IAV and RSV replication at the post-entry stage[1].
Sakuranetin is a rice flavonoid phytoalexin, shows strong antifungal activity[1]. Sakuranetin has anti-inflammatory and antioxidative activities. Sakuranetin ameliorates LPS-induced acute lung injury[2].
[5-(2-Thienyl)-3-isoxazolyl]methanol (Compound D) is an AgrA-DNA binding inhibitor. [5-(2-Thienyl)-3-isoxazolyl]methanol can be used for S.aureus infection research[1].
Antioxidant agent-9 is a peptide with the sequence Asp-Trp. Antioxidant agent-9 shows antioxidant activity. Antioxidant agent-9 also is potential as SARS-CoV-2 antiviral, with an affinity strength equal to Chloroquine (HY-17589A) and Favipiravir (HY-14768)[1][2].
Angustifoline, an alkaloid, can be isolated from Lupinus angustifolius L. alkaloid extract. Angustifoline exhibits antimicrobial activity. Angustifoline could have bacteriostatic effects against S. aureus, B. subtilis, E. coli, P. aeruginosa and B. thuringiensis[1].
Teicoplanin sodium (Antibiotic MDL-507 sodium) is a potent lipoglycopeptide antibiotic. Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity[1][2].
Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth[1][2].
Dihydrostreptomycin sulfate is an aminoglycoside antibiotic, used to treat bacterial diseases in cattle, pigs and sheep.
(+)-Magnoflorine (Magnoflorine) is an aporphine alkaloid found in Acoruscalamus, with anti-fungal activity, reduces the formation of C. albicans’ biofilm[1]. Anti-antidiabeticand anti-oxidative activity[2].
Bofutrelvir (FB2001) is a SARS-CoV-2 main protease Mpro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077)[1][2].
Thiolactomycin is an antibiotic. Thiolactomycin is active against Gram-negative anaerobes. Thiolactomycin also inhibits malaria and trypanosomes. Thiolactomycin is a FabB inhibitor. Thiolactomycin inhibits the synthesis of fatty acids and mycolic acids[1][2].
HBV-IN-29 (ex8), a flavone derivative, is a potent covalently closed circular DNA (cccDNA) inhibitor. cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-29 has the potential for the research of HBV infection[1].
Framycetin (Fradiomycin B; Neomycin B) is an aminoglycoside antibiotic. It inhibits hammerhead ribozyme with a Ki of 13.5 μM.
BMS-538203 is a highly efficient HIV integrase inhibitor and antiviral agent.IC50 value:Target: HIV integraseIn the current study we demonstrate a hit-to-clinical candidate pathway that resulted in 50- and 2000-fold improvements in enzyme-inhibition and antiviral activity without an increase in molecular weight or change in molecular topology. The original hit , 1 (mw = 268) was optimized in a stepwise manner. Potential covalent protein-binding moieties were removed by reducing the number of the ketone groups. High enzyme inhibition activity was achieved by optimizing the aryl-portion of the molecule. Protein binding was reduced by replacing the standard amide by the corresponding methyl-hydroxamide. This eventually led to the discovery of BMS-538203 compound 2 (mw = 269) a highly efficient inhibitor and antiviral agent.
Influenza A virus-IN-5 (Compound 16e) is a potent, orally active anti-influenza A virus (IAV) agent with an IC50 of 1.29 μM. Influenza A virus-IN-5 inhibits the transcription and replication of viral RNA with acceptable cytotoxicity[1].
Enterocin Hybrid 1 is a antibacterial agent, a antibacterial composition. Enterocin Hybrid 1 inhibits Vancomycin (HY-B0671)-resistant E. faecium, Staphylococcus haemoliticus[1].
Lincomycin Hydrochloride(U10149A) is an antibiotic produced by Streptomyces lincolnensis var. lincolnensis.Target: AntibacterialLincomycin hydrochloride is a systemic antibiotic, which is active against most common gram positive bacteria. It has proved to be excellent for infectious diseases like acne, anthrax, pneumonia, and also for the treatment of furunculosis, carbuncles, impetigo, burns and wounds, carrying to gram positive bacteria. Lincomycin hydrochloride inhibits cell growth and microbial protein synthesis, by interacting strongly and specifically with the 50S ribosomal subunit, at mutually related sites [1-3].
Quinine Hydrochloride Dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste.Target: AntiparasiticQuinine is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), and anti-inflammatory properties and a bitter taste. It is a stereoisomer of quinidine, which, unlike quinine, is an antiarrhythmic. Quinine contains two major fused-ring systems: the aromatic quinoline and the bicyclic quinuclidine. In patients with cerebral malaria receiving the standard dose of 10 mg/kg every eight hours, plasma quinine concentrations consistently exceeded 10 mg/liter, reaching a peak 60 ± 25 hours (mean ± 1 S.D.) after treatment was begun and then declining. Quinine total clearances (CI) and total apparent volumes of distribution (Vd) were significantly lower than in uncomplicated malaria (CI, 0.92 ± 0.42 compared with 1.35 ± 0.6 ml/min/kg, p = 0.03; Vd, 1.18 ± 0.37 compared with 1.67 ± 0.34 liter/kg, p = 0.0013) [1].
Atazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor.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