Posaconazole-D4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
Mycothiol is a major low molecular-mass thiol that exists in mycobacteria. Mycothiol is an intracellular reducing agent[1].
Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
Antifungal agent 36 is a potent anti-fungal agent. Antifungal agent 36 shows anti-fungal activity for Basidiomycetes[1].
Pefloxacin mesylate dehydrate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Levomecol (Chloramphenicol), made up of Chloramphenicol, Methyluracil, is a broad-spectrum antibiotic that is derived from the bacterium Streptomyces venezuelae. Levomecol (Chloramphenicol)) stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis[1].
Kasugamycin is an important amino-glycoside family antibiotic and widely used for veterinary and agricultural applications.
Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbenoids and coumarin[1]. Coniferyl alcohol specifically inhibits fungal growth[1].
Berteroin, a naturally occurring Sulforaphane analog, ia an antimetastatic agent. Berteroin has anti-inflammatory, antitumor and bactericidal effects[1][2].
Antiviral agent 20 (Compound 17b) is a selective inhibitor against Zika virus infection with an EC50 of 4.5 µM. Antiviral agent 20 has low cytotoxicity[1].
Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective[1].
2-Phenylethanol-d9 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.
Indinavir sulfate(MK-639 sulfate; L735524 sulfate ) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated [1]. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom [2].
Antibacterial agent 42, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Odesivimab is a humanized monoclonal antibody, targeting Ebola virus glycoprotein with a KD value of 7.74 nM for recombinant histidine-tagged Makona strain Ebola virus glycoprotein ectodomain protein. Odesivimab can be used in research of Ebola virus infection[1].
Camalexin is a phytoalexin isolated from Camelina sativa and Arabidopsis (Cruciferae) with antibacterial, antifungal, antiproliferative and anticancer activities. Camalexin can induce reactive oxygen species (ROS) production[1][2][3].
Cap-dependent endonuclease-IN-20 is a cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-20 shows antiviral activity against influenza virus A/Hanfang/359/95 (H3N2) with IC50 of 4.82 μM (CN112940009A; DSC801)[1].
Mtb-IN-4 (compound 17h) is a nontoxic isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity (IC50=0.70 μM). Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant[1].
Benzisothiazolinone-13C5 (1,2-Benzothiazol-3-one-13C5) is a 13C-labeled Benzisothiazolinone. Benzisothiazolinone is widely used as an antiseptic and antibacterial agent[1].
Urease-IN-7 (Compound 5k) is a competitive Urease inhibitor (IC50: 3.33 μM, Ki: 3.62 μM). Urease-IN-7 can be used for research of peptic and gastric ulcers[1].
Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicans, C. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae)[1][2].
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.
Antiviral agent 30 (Example 118) is an antiviral agent. Antiviral agent 30 is active against HCV and RSV (IC50: > 25μM)[1].
2,5-Dihydroxybenzaldehyde (Gentisaldehyde) is a naturally occurring antimicrobial that inhibits the growth of Mycobacterium avium subsp. paratuberculosis. 2,5-Dihydroxybenzaldehyde is active against S. aureus strains with a MIC50 of 500 mg/L[1][2].
Pseudin-2, an AMP thast could be isolated from the skin of the South American paradoxical frog Pseudis paradoxa, exert a potent growth inhibitory effect against Gram-negative bacteria[1].
Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease[3].
Sulfathiazole is an organosulfur compound that has been used as a short-acting sulfa drug.Target: AntibacterialSulfathiazole (20 μg/L) starts to be degraded between day 31 and day 38 in one of the two batch reactors containing different wastewater matrices. Sulfathiazole is degraded at a substantially faster rate than sulfamethoxazole or sulfamethazine in the nitrification process (S3) [1]. Recovery from spiked manure slurry samples is 64% for Sulfathiazole at pH 9. Sulfathiazole has acidity constant of pKa of 7.1and retention times (tR) of 7.8. S/N values for Sulfathiazole are above 100 at the 1 mg/kg level [2]. Sulfathiazole sorption to inorganic sorbents exhibits pronounced pH dependence consistent with sorbate speciation and sorbent charge properties. Sulfathiazole cations are most important for sorption to clay minerals, followed by neutral species [3].
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves[1].
Merafloxacin (CI-934), a fluoroquinolone antibacterial agent, is a selective programmed -1 ribosomal frameshifting (-1 PRF) inhibitor of beta coronaviruses. Merafloxacin exhibits in vitro activity against gram-positive and gram-negative bacteria[1][2].
Zoxamide (RH-7281) is an oomycete fungicide. Zoxamide arrests nuclear division in Phytophthora capsici germlings and destroyed the microtubule cytoskeleton[1][2].