Varioxepine A is a 3H-oxepine-containing alkaloid with a new oxa-cage found in the marine algal-derived endophytic fungus Paecilomyces variotii. Varioxepine A inhibits plant pathogenic fungus Fusarium graminearum[1].
Duramycin (Moli1901;Lancovutide) is a cyclic peptide lantibiotic derived from Streptomyces cinnamoneuma. Duramycin stimulates chloride secretion in airway epithelium and has the potential for cystic fibrosis treatment. Duramycin interacts with phosphatidylethanolamine (PE) and has antibacterial, antiviral effects[1][2].
Efrotomycin is an orally active antibiotic. Efrotomycin can be isolated from the Streptomyces Lactamdurans. Efrotomycin has insignificant effect on Salmonella typhimurium quantity, duration, shedding rate, and antimicrobial susceptibility in infected pigs[1][2].
Norstictic acid is a potent and selective allossteric transcriptional regulator. Norstictic acid shows anticancer activity. Norstictic acid shows antioxidant activity and antimicrobial activity[1][2][3][4].
8CN, a 2-amino-thiophene derivative, has anti-leishmanial activity. 8CN can be used in research of Leishmaniasis[1].
Omadacycline is a new tetracycline antibiotic in the pipeline, which can inhibit the 30s subunit of bacterial ribosome.IC50 Value:Target: Antibacterialin vitro: in vivo: Clinical trial: Phase III Study to Compare the Safety and Efficacy of PTK-0796 in Patients With Complicated Skin and Skin Structure Infection (CSSSI).
Urtoxazumab (TMA-15) is a humanized monoclonal antibody against Shiga toxin (Stx) 2[1].
Vincetoxicoside B, isolated from Polygonum paleaceum Wall, shows antifungal activity[1].
L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
Lauryl-LF 11, N-terminally acylated analogue of LF11, is a peptide with antibacterial activity[1].
Danofloxacin Mesylate(CP76136-27 mesylate) is a fluoroquinolone antibacterial for veterinary use.Target: AntibacterialDanofloxacin is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase, which is necessary for supercoiling of DNA to provide a suitable spatial arrangement of DNA within the bacterial cell. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, is 0.125 μg/ml [1]. Danofloxacin shows protective dose (PD50) of 0.38, 0.8, 2.42 mg/kg for P. multocida, E. coli and S. choleraesuis in in vivo mouse protection assay [2].
LASV inhibitor 3.3 (LAMP1 inhibitor 3.3) is a specific inhibitor of Lassa fever virus (LASV, IC50=1.8 uM), inhibits LASV GP-mediated infection and cross-links to the LASV receptor, LAMP1, in cells; does not inhibits the GP-mediated infection of LCMV, LuJo virus (LUJV) or Junin virus (JUNV), Ebola virus (EBOV) or vesicular stomatitis virus (VSV); inhibits LAMP1 binding to LASV GP, which is cholesterol-dependent and sensitive to 3.3 inhibition; LASV inhibitor 3.3 is a competitive inhibitor of cholesterol binding to LAMP1.
Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively[1].
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice[1].
SARS-CoV-2-IN-39 (compound 21) is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 against SARS-CoV-2 by inhibiting of SKP2 protein and stabilizing BECN1[1].
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability[1].
RRx-001 is a potent inhibitor of G6PD. RRx-001 shows potent antimalarial, although as a single agent, the drug sensitivity testing indicated that higher dose of RRx-001 was required to inhibited 50 % of the parasite's activity (IC50 = 0.14 ± 0.04 ug/ml).IC50 value: 0.14 ± 0.04 ug/ml [1]Target: G6PDin vitro: RRx-001 is a novel, systemically non-toxic, epigenetic anticancer agent for multiple tumour types, with activity mediated through increased nitric oxide (NO) production and PPP inhibition. [1]in vivo: RRx-001is a novel, nonexplosive molecule modified from a class of solid rocket propellants, has shown promise as a novel cancer therapeutic agent in a number of cell lines and tumor models. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. [2]
Dimetridazole-d3 (1,2-Dimethyl-5-nitroimidazole-d3) is a deuterium labeled Dimetridazole. Dmetridazole, a nitroimidazole-based antibiotic, combats protozoan infections[1].
Anhydrotetracycline shows dose-dependent and potent inhibition of tetracycline destructases in vitro[1].
Benzoic acid-d5 is a deuterium substitute for Benzoic acid. Benzoic acid is an aromatic alcohol that occurs naturally in many plants and is a common additive in food, beverages, cosmetics and other products. Benzoic acid can act as a preservative by inhibiting bacteria and fungi[1][2].
Antileishmanial agent-10 (Compound 7h) is an antiprotozoal agent[1].
β-?Solamarine is an antibacterial agent[1].
7-Methoxy-β-carboline-1-propionic acid (compound 46) is a cytotoxic and antimalarial compound. 7-Methoxy-β-carboline-1-propionic acid can be extracted from the roots of Eurycoma longifolia[1].
Anti-infective agent 1 (compound 3a) is a potent and selective antiprotozoal and antimycobacterial agent. Anti-infective agent 1 shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 10.95 and 0.06 μM, respectively. Anti-infective agent 1 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 8 μg/mL[1].
Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively.
Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions[1]. Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages[2].
SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.
Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine. IC50 value:Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A base pairs and a bulged-out adenine. The binding mode of apramycin at the human decoding-site RNA is distinct from aminoglycoside recognition of the bacterial target, suggesting a molecular basis for the actions of apramycin in eukaryotes and bacteria.
Cloxacillin sodium exhibits antibiotic efficacy, with a MIC of 256 mg/L for Staphylococcus aureus 25923[1][2][3].
Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.