Temporin F is an antimicrobial peptide against Legionella pneumophila[1].
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity[1][2][3][4][6].
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs)[1].Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy[2].
Bacitracin is a polypeptide antibiotic used for staphylococcal infections. Bacitracin functions as an inhibitor of cell wall biosynthesis through its binding to the undecaprenyl pyrophosphate. The combination of bacitracin with other antibiotics has been efficient to be used as a topical agent[1].
Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect[1][2][3][4][5][6][7].
A small molecule with activity against drug-resistant and persistent tuberculosis; shows bactericidal activity against nonreplicating Mtb in vitro and is efficacious in acute and chronic Mtb infection mouse models; down-regulates genes known to be involved in Mtb persistence; inhibits DprE1 and MoeW, enzymes involved in cell wall and molybdenum cofactor biosynthesis.
Tenofovir-C3-O-C15-CF3 (ammonium) exhibits substantially longer t1/2 values than tenofovir in human liver microsomes, potent anti-HIV activity in vitro, and enhances pharmacokinetic properties in vivo.
Dixanthogen is an ectoparasiticide.
Xanthoangelol, extracted from Angelica keiskei, suppresses obesity-induced inflammatory responses. Xanthoangelol possesses antibacterial activity[1][2]. Xanthoangelol and inhibits monoamine oxidases[3]. Xanthoangelol induces apoptosis in neuroblastoma and leukemia cells[4].
Clavulanic acid is a naturally occurring powerful bacterial β-lactamases inhibitor for research of infections caused by bacteria, including infections of the ears. Clavulanic acid is active against a wide spectrum of gram-positive and gram-negative bacterias[1].
Casirivimab (REGN10933) is a human monoclonal antibody to target SARS-CoV-2 virus, which causes COVID-19. Casirivimab lacks efficacy against COVID-19 variants. Casirivimab can be used in combination with Imdevimab (HY-P99342), it reduces viral load and improves diseases[1].
Monascorubramine is a microbial colorant. Monascorubramine is capable of producing by the Monascus, which is from the bacteria Talaromyces. Under the condition of different pH value, the hue and chromaticity value of the colorant are also different[1].
TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.
R-1479 is a specific inhibitor of HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).
Ingenol-3-palmitate, an ingenane diterpenoid, is a nature product that could be isolated from the roots of Euphorbia ebracteolata. Ingenol-3-palmitate is a potent HIV-1 (HIV) inhibitor with an IC50 value of 4.1 nM[1].
(E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as green onion (Allium cepa) or noni (Morinda citrifolia L.) leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
Cefacetrile (Cephacetrile) is a broad-spectrum antibiotic that is effective in gram-positive and gram-negative bacterial infection[1][2].
Collinin is a anti-tubercular agent, it can be isolated from leaves of Z. schinifolium. Collinin has an excellent anti-tuberculosis effect against multidrug-resistant (MDR), extensively drug-resistant (XDR) strains[1].
Oxazosulfyl is a potent agricultural fungicide. Oxazosulfyl can be used as an insecticide against major rice pests[1].
Meridinol ((-)-Meridinol) shows antimicrobial activity against a wide range of gram-positive and gram-negative bacteria and fungi.
Solithromycin is a novel fluoroketolide with improved antimicrobial effectiveness.Target: AntibacterialSolithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. The mean 50% inhibitory concentrations (IC50s) for Solithromycin inhibition of cell viability, protein synthesis, and growth rate were 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae,Staphylococcus aureus, and Haemophilus influenzae, respectively.
LeuRS-IN-1 is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively[1]. LeuRS-IN-1 inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM)[2].
Tunicamycin V (Tunicamycin A) is a nucleoside natural product that inhibits bacterial phospho-N-acetylmuramyl-pentapeptide transferase (MraY) with an IC50 of 0.35 μM. Tunicamycin V has antibacterial activties[1][2].
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities[1][2].
Carvacrol methyl ether, a Carvacrol analog, can be isolated from plant volatile oil. Carvacrol methyl ether exhibits antibacterial activity[1][2].
(R)-Edelfosine ((R)-ET-18-OCH3) is a ether lipid analog with anti-HIV and antineoplastic activity[1].
Thiophanate-methyl-d6 is the deuterium labeled Thiophanate-methyl. Thiophanate-Methyl is a systematic fungicide[1][2].
Rimocidin, a polyene macrolide, is an antifungal compound. Rimocidin shows broad‐spectrum antifungal activity against multiple plant‐pathogenic fungi[1][2].
Pyrimethamine(RP4753) is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).IC50 Value: 15.4 nM (Plasmodium falciparum) [1]Target: DHFR; antifolatein vitro: Three susceptibility levels (susceptible, intermediate, and resistant) were observed in the response of culture-adapted clones and strains to pyrimethamine (50% inhibitory concentration [IC50]) < 100, 100-2,000, and > 2,000 nM) and cycloguanil (IC50 < 50, 50-500, and > 500 nM). Based on these susceptibility levels, 73 and 68 of 96 fresh clinical isolates were susceptible to pyrimethamine (mean IC50 15.4 nM) and cycloguanil (mean IC50 11.1 nM), respectively [1]. We tested pyrimethamine(previously reported to suppress SOD1 expression), several compounds currently in trials in human and murine ALS, and a set of 1040 FDA-approved compounds. In a PC12 cell-based assay, no compounds reduced SOD1 promoter activity without concomitant cytotoxicity. Additionally,pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice [3].in vivo: (131)I-Pyrimethamine (specific activity: 7.08 MBq/ mol) was injected intravenously into the tail vein of the control and infected rats. Static whole body images of the rats were acquired under the gamma camera at 5 min, 45 min, 2 h, 6 h, and 24 h following the intravenous administration of the radioactivity (3.7 MBq/rat) [2]. The 10-day treatment with 10mg/kg/day of fluconazole combined with 40/1mg/kg/day sulfadiazine and pyrimethamine resulted in 93% survival of CF1 mice acutely infected with the highly virulent T. gondii RH strain, versus 36% of mice treated with just sulfadiazine and pyrimethamine [4].Toxicity: Sulfadoxine/pyrimethamine is well tolerated as treatment and when used as intermittent preventive treatment in pregnant African women. Sulfadoxine/pyrimethamine is no longer used as prophylaxis because it may cause toxic epidermal necrolysis and Stevens Johnson syndrome [5].
2-Heptanol is one of chemical constituents identified in the essential oil of rhizome of Curcuma angustifolia and Curcuma zedoaria. Rhizome essential oil exhibited good antimicrobial and antioxidant activity[1].