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.
Atherosperminine（Atherospermine）is a nature occurring alkaloid, has antiplasmodial activities in vitro, with an IC50 of 5.80 μM. Atherosperminine is good reductants with the ability to chelate metals and presented pro-oxidant activity. Atherosperminine exerts a non-specific relaxant effect on the trachealis[1].
(+)-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].
IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis[1].
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitory activity against HIV-1 protease, with IC50 >100 μg/mL[1].
Antiparasitic agent-6 (compound 5b) has selectively antiparasitic activity against Leishmania infantum (L. infantum) with an IC50 value of 3.89 μM. Antiparasitic agent-6 also has certain cytotoxicity against HepG2 (CC50 = 13.64 μM)[1].
Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity[1].
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].
Glu-Ala-Leu-Phe-Gln-pNA is a Chiba virus 3C-like protease (CVP) substrate[1].
Celestine Blue is a electroactive indicator in DNA biosensors. Celestine Blue is strongly adsorbed on the spinel phases and CNT (carbon nanotubes), facilitates dispersion, acts as a capping agent and allows for the fabrication of spinel decorated CNT. Celestine Blue is an efficient charge transfer mediator, which allows for significant improvement of capacitive behavior. TiO2 nanoparticles doped with Celestine Blue can be used as a label in a sandwich immunoassay for the hepatitis C virus (HCV) core antigen[1][2][3].
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].
7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake (IC50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC50s of 1.18 μM and 0.97 μM, respectively[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
(E)-β-Farnesene (trans-β-Farnesene) is a volatile sesquiterpene hydrocarbon which can be found in Phlomis aurea Decne essential oil. (E)-β-Farnesene can be used as a feeding stimulant for the sand fly Lutzomyia longipalpis[1][2].
IHVR-19029 is a novel antiviral compound that acts as ER α-glucosidase inhibitor, synergistically inhibits the replication of Yellow fever and Ebola viruses in cultured cells combined with favipiravir (T-705); significantly increases the survival rate of infected animals in mouse model of Ebola virus infection.
Carviolin is a compound isolated from the mycelia of the ascomycete Neobulgaria pura. Carviolin inhibits the formation of appressoria in germinating conidia of Magnaporthe grisea on inductive (hydrophobic) surface. Carviolin exhibits moderate cytotoxic, but no antifungal, antibacterial, or phytotoxic activities[1].
Cerbinal is a natural compound isolated from Gardenia jasminoides Ellis. Cerbinal has antifungal activity[1].
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistant K. pneumoniae. K11 has high thermal and wide pH stability[1].
Cinerubin B, a glycosylated anthracycline antibiotic, is an anticancer agent from Streptomyces sp. SPB74[1].
H-Trp-Trp-Trp-OH is a tripeptide consisting of tryptophan. H-Trp-Trp-Trp-OH has antibacterial activity[1].