1,4, 6-trihydroxy-5-methoxy-7-prenylxanthone is an antimicrobial agent that can be isolated from the genus garcinia. 1,4, 6-trihydroxy-5-methoxy-7-prenylxanthone inhibits S. aureus and B. cereus with MIC values of 128 μg/mL and 200 μg/mL, respectively[1].
Fumaramidmycin is an antibiotic found in Streptomyces kurssanovii NR-7GG1. Fumaramidmycin shows an antimicrobial activity against both Gram-positive and Gram-negative bacteria[1].
PXYD3 is a ribosomal protein S1 (RpsA) antagonist with Kds of 5.66 and 6.91 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
Mequindox is an antimicrobial agent[1]. Mequindox acts as an inhibitor of DNA synthesis. Mequindox induces genotoxicity and carcinogenicity in mice[2].
Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible and competitive broad-spectrum inhibitor of metallo-β-lactamases (MβLs), with IC50s of 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM for L1, ImiS, IMP-1 and VIM-2, respectively. Metallo-β-lactamase-IN-8 exhibits antibacterial activity[1].
Methasulfocarb is a fungicide compound.
Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract and malarial infections.Target: AntiparasiticSulfadoxine(Sulphadoxine) is an ultra-long-lasting sulfonamide. Sulfadoxine is often used in combination with pyrimethamine to treat or prevent malaria. Both drugs are antifolates; they inhibit the production of enzymes involved in the synthesis of folic acid within the parasites. Either drug by itself is only moderately effective in treating malaria, because the parasite Plasmodium falciparum may be able to use exogenous folic acid, i.e. folic acid which is present in the parasite's environment, while in combination, the two substances have a synergistic effect which outbalances that ability [1, 2].
Leachianone G is an antiviral flavonoid from the root bark of Morus alba L. Leachianone G shows potent antiviral activity against herpes simplex type 1 virus (HSV-1) with an IC50 value of 1.6 μg/mL[1].
Destomycin B (A-16316-C) is an antibiotic, and is active against fungi. Destomycin B also has anthelmintic activity[1].
Ceftriaxone is an antibiotic useful for the treatment of a number of bacterial infections.Target: AntibacterialCeftriaxone inhibits bacterial cell wall synthesis by means of binding to the penicillin-binding proteins (PBPs). Inhibition of PBPs would in turn inhibit the transpeptidation step in peptidoglycan synthesis which is required for bacterial cell walls. Like other cephalosporins, ceftriaxone is bacteriocidal and exhibits time-dependent killing. Ceftriaxone, one of the beta-lactam antibiotics, is a stimulator of EAAT2 expression with neuroprotective effects in both in vitro and in vivo models based in part on its ability to inhibit neuronal cell death by glutamate excitotoxicity. Based on this consideration and its lack of toxicity, ceftriaxone has potential to manipulate glutamate transmission and ameliorate neurotoxicity [1].
Maximin 4 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 4 has cytotoxicity on tumor cells and spermicidal effect[1].
Anpocogin is the Ancyclostoma canium nematode anticoagulant protein c2, variant (C-terminal P85 added). Anpocogin, produced in Pichia pastoris, serves as an anticoagulant agent[1].
Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Cowaxanthone B is a xanthone isolated from the fruits of Garcinia cowa. Cowaxanthone B has weak antibacterial activity[1].
Genkwanol C, a biflavonoid, has effective antiviral activity against respiratory syncytial virus (RSV) in vitro[1].
HIV-IN-4 (Compound 12) is a potent inhibitor of HIV. HIV-IN-4 shows promising anti-HIV activities[1].
Norfloxacin-d5 is a deuterium labeled Norfloxacin. Norfloxacin is a fluoroquinolone antibiotic that inhibits the growth of Gram-positive and Gram-negative bacteria (MICs = 4 μg/mL and 1 μg/mL for S. aureus and P. aeruginosa, respectively). Norfloxacin also inhibits the growth S. pseudintermedius, S. aureus, E. coli, Pasturella, and S. canis isolates from dogs (mean MIC50s = 0.25 μg/mL, 1 μg/mL, 0.03 μg/mL, 1 μg/mL, and 1 μg/mL, respectively).
Azathramycin is an antibiotic.
(±)-Heraclenol, a coumarin, is isolated from the fruits of Angelica lucida, and exhibits antibacterial activities[1].
HBV-IN-31 is a potent cccDNA (covalently closed circular DNA) inhibitor. HBV-IN-31 shows anti-HBV activity with an IC50 value of 0.13 µM for HBsAg. HBV-IN-31 inhibits cell growth[1].
PF-232798 is an orally active CCR5 antagonist with anti-HIV effects[1].
Arbidol (Umifenovir) hydrochloride is an broad-spectrum antiviral chemical agent which can inhibit cell entry of enveloped viruses by blocking viral fusion with host cell membraneIC50 value:Target: Antiviral; Anti-influenza agentin vitro: Arbidol was found to present potent inhibitory activity against enveloped and non-enveloped RNA viruses, including FLU-A, RSV, HRV 14 and CVB3 when added before, during, or after viral infection, with 50% inhibitory concentration (IC50) ranging from 2.7 to 13.8 microg/ml.However, arbidol showed selective antiviral activity against AdV-7, a DNA virus, only when added after infection (therapeutic index (TI) = 5.5) [1]. Arb interacts with the polar head-group of phospholipid at the membrane interface. Fluorescence studies of interactions between Arb and either tryptophan derivatives or membrane peptides reconstituted into liposomes show that Arb interacts with tryptophan in the micromolar range. Interestingly, apparent binding affinities between lipids and tryptophan residues are comparable with those of Arb IC50 of the hepatitis C virus (HCV) membrane fusion [2]. Arbidol not only prevented the cytopathic effect (CPE) of CVB(5), as demonstrated in an MTT colorimetric assay, when added during or after viral infection, with a 50% inhibitory concentration (IC(50)) from 2.66 to 6.62 microg/ml, but it also decreased the CVB(5)-RNA level in infected host cells, as shown in semi-quantitative RT-PCR [3].in vivo: Orally administered arbidol at 50 or 100 mg/kg/day beginning 24 h pre-virus exposure for 6 days significantly reduced mean pulmonary virus yields and the rate of mortality in mice infected with FLU-A (A/PR/8/34 H1N1) [1]. BALB/c mice were used as an animal model to test the Arbidol activity in vivo. Orally administered Arbidol at 50 mg/kg body weight/day (once a day) significantly reduced mean virus yields in the lungs and heart as well as mortality after infection for 6 days [3].
Azoxystrobin is a broad-spectrum β-methoxyacrylate fungicide. Azoxystrobin inhibits mitochondrial respiration by binding to the Qo site of the cytochrome bc1 complex and inhibiting electron transfer. Azoxystrobin induces the production of reactive oxygen species (ROS) and induces cell apoptosis.
Oxytetracycline is a tetracycline analog isolated from the actinomycete streptomyces rimosus and used in a wide variety of clinical conditions.Target: AntibacterialOxytetracycline was the second of the broad-spectrum tetracycline group of antibiotics to be discovered. Oxytetracycline works by interfering with the ability of bacteria to produce essential proteins. Without these proteins, the bacteria cannot grow, multiply and increase in numbers. Oxytetracycline therefore stops the spread of the infection and the remaining bacteria are killed by the immune system or eventually die.Oxytetracycline is a broad-spectrum antibiotic, active against a wide variety of bacteria. However, some strains of bacteria have developed resistance to this antibiotic, which has reduced its effectiveness for treating some types of infections [1, 2].
Ethyl acetoacetate-13C is the 13C labeled Ethyl acetoacetate[1]. Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[2][3][4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[5].
IMB-26 is a HCV inhibitor with an EC50 of 2.1 μM. IMB-26 shows potent an anti-HCV activity[1].
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM)[1]. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM[2].
Orysastrobin, a “quinone outside inhibitor” (QoI)-type fungicide, has excellent fungicidal efficacy against leaf and panicle blast and against sheath blight in rice[1].
SARS-CoV-2-IN-31 is an effective COVID-19 inhibitor. SARS-CoV-2-IN-31 exhibits excellent to mild activity against various cancer cell lines with IC50 values range from 28.84 to 38.36 μM. SARS-CoV-2-IN-31 can be used for the research of cancer[1].
Cefoxitin sodium (MK-306) is a cephamycin antibiotic, often grouped with the second generation cephalosporins, acts by interfering with cell wall synthesis, its activity spectrum includes a broad range of gram-negative and gram-positive bacteria.