Isopsoralenoside is a benzofuran glycoside from Psoralea corylifolia. Isopsoralenoside can be quickly metabolized to Psoralen (HY-N0053) in digestive tract contents. Isopsoralenoside show estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity[1].
Cefoselis is a widely used beta-lactam antibiotic.Target: AntibacterialCefoselis, a new parenteral cephalosporin, was active against clinical isolates of both gram-positive and gram-negative aerobic bacteria. The activity of Cefoselis was similar to that of cefpirome and cefepime and generally superior to that of ceftazidime. Cefoselis showed potent antibacterial activity against Hemophilus influenzae and Moraxella catarrhalis.Cefoselis was highly active against MSSA and MSCNS. Cefoselis was poor in the activity against MRSA,MRCNS,PRSP and Enterococcus faecalis,and no activity for Enterococcus faecium.
TH-Z93, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 90 nM)[1].
Pardaxin P5 is an antimicrobial peptide that inhibits Escherichia coli with a MIC value of 13 μM[1].
1-Naphthalenemethanol is a natural compound the root bark extracts of Annona senegalensis with antibacterial activity[1].
DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase[1][2].
Emetine hydrochloride, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine hydrochloride inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine hydrochloride potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect[1][2][3][4].
Temporin K is an antimicrobial peptide against Legionella pneumophila[1].
4(1H)-Quinolinone, 1-methyl-2-(5Z)-5-undecen-1-yl- (compound 2) is a quinolone alkaloid that can be isolated from Cnidium. 4(1H)-Quinolinone, 1-methyl-2-(5Z)-5-undecen-1-yl- has methicillin-resistant Staphylococcus aureus (MRSA) activity, with MIC values of 32 μg/mL (ATCC 33591) and 16 μM/mL (ATCC 25923), respectively[1].
I2906 showed antimycobacterial and cytotoxic activity against mycobacterium tuberculosis.IC50 Value: Target: AntibacterialUnder in vitro conditions, I2906 showed excellent antimycobacterial activities and low cytotoxicity. In a murine model infected with M. tuberculosis H37Rv, the reductions on bacterial loads of both lungs and spleen were statistically significant (p < 0.05) between I2906-treated mice and untreated controls after 4 weeks. Further, the colony-forming unit counts in the lungs were dramatically lower (p < 0.05) than that of isoniazid-treated mice by the addition of I2906 after 8 weeks. Moreover, survival rate was increased by I2906 treatment. For multidrug-resistant strain infection, bacterial counts were reduced significantly in the lungs and spleen due to I2906 treatment in comparison with data from untreated controls (p < 0.05).
Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment. Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer[1].
Obtusalin is a triterpenoid found in R. dauricum for the first time and shows UV absorption at 210 nm. Obtusalin has some antibacterial activity[1][2].
Piperacillin is kind of semisynthetic penicillins. Piperacillin has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Piperacillin has shown greater activity against β-lactamase-producing organisms than the other penicillins[1].
Fleroxacin is a broad-spectrum antimicrobial fluoroquinolone.Target: AntibacterialFleroxacin (Ro 23-6240; AM-833) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg) [1]. Fleroxacin is effective against Haemophilus ducreyi in vitro. Fleroxacin, 200 or 400 mg as a single oral dose, is efficacious therapy for microbiologically proven chancroid in patients who do not have concurrent HIV-1 infection. Among HIV-1-infected men, a single dose of 200 or 400 mg of fleroxacin is inadequate therapy for chancroid [2, 3].
Isobavachromene is an antibacterial agent[1].
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies[1][2][3].
Isoeugenol is an essential oil constituent of nutmeg, clove, and cinnamon. Isoeugenol inhibits growth of Escherichia coli and Listeria innocua with MICs of 0.6 mg/mL and 1 mg/mL, respectively[1].
Pinocembrin chalcone (2',4',6'-Trihydroxychalcone) is an antibacterial compound from Helichrysum Trilineatum. Pinocembrin chalcone can prevent gastric ulcers in rats[1].
Antibacterial agent 158 (compound 6c), a Micrococcin analogue, and is effective against impetigo and C. difficile infection (CDI)[1].
β-Lactamase-IN-5 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 720. β-Lactamase-IN-5 can be used for the research of bacterial infections[1].
Furomollugin is a natural product with antioxidant and antibacterial activities, can be isolated from Rubia cordifolia. Furomollugin lacks potent anti-tyrosinase activity, but also exhibits significant anticancer property[1].
2-Phenylethanol-d5 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Squalamine(MSI-1256) is an aminosterol compound with potent broad spectrum antiviral activity.IC50 value: Target: in vitro: squalamine can strongly displace membrane-bound cationic proteins such as Rac1, a ρ-GTPase recruited to the inner leaflet of the eukaryotic cytoplasmic membrane for the actin remodeling necessary for endocytosis. At concentrations between 20 and 60 μg/mL, squalamine has been shown to inhibit a broad array of growth factor-induced, actin-dependent responses in endothelial cells, including cell migration, cell division, and vascular tube formation in a 3D matrix [1]. Squalamine effectively inhibited HBV replication in human primary hepatocytes when added either during the initial exposure of virus to the cells or at 24 h after infection. A similar study was performed to evaluate the effect of squalamine on the replication of HDV. Squalamine was introduced at 20 μg/mL during HDV exposure, and the effects were measured at day 7 when total RNA was extracted and assayed for HDV RNA sequences [1]. in vivo: one time daily treatment with squalamine (15 or 30 mg/kg per d s.c.) was started beginning on day 1 or 2 after viral administration and continuing until day 8 or 9, respectively. Survival was monitored, and animals that remained alive by day 21 were considered cured [1].
4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
Actinomycin D inhibits DNA repair with an IC50 of 0.42 μM.
Temporin L is a potent antimicrobial peptide and is active against Gram-negative bacteria and yeast strains. Temporin L also has antiendotoxin properties[1][2].
Cefalonium is the first-generation β-lactam cephalosporin antibiotic that is widely used to research bovine mastitis caused by Gram-positive bacteria including staphylococci[1][2][3].
Eugenol is an essential oil found in cloves with antibacterial, anthelmintic and antioxidant activity. Eugenol is shown to inhibit lipid peroxidation.
Gageotetrin B has antimicrobial activities. Gageotetrin B is more active against fungi compared to bacteria with MIC values of 0.01-0.04 μM[1].
(+)-Medioresinol is a furofuran type lignan with antifungal, antibacterial and lesishmanicidal activities. (+)-Medioresinol leads to intracellular ROS accumulation and mitochondria-mediated apoptotic cell death in Candida albicans. (+)-Medioresinol can reduce the cardiovascular disease risk[1][2].