Norfloxacin hydrochloride is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.Target: DNA gyrase; AntibacterialNorfloxacin is a synthetic chemotherapeutic antibacterial agent occasionally used to treat common as well as complicated urinary tract infections. Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.There are currently three approved uses in the adult population (one of which is restricted) and the other ineffective due to bacterial resistance. Chibroxin (ophthalmic) is approved for use in children older than one year of age.Norfloxacin is associated with a number of rare serious adverse reactions as well as spontaneous tendon ruptures and irreversible peripheral neuropathy. Tendon problems may manifest long after therapy had been completed and in severe cases may result in lifelong disabilities. Hepatoxicity resulting in fatalities has also been reported with the use of norfloxacin.
ClpB-IN-1 (compound 7) is a potent ClpB inhibitor[1].
Antifungal agent 77 (Compound 13h) is an antifungal agent. Antifungal agent 77 (500 μg/mL) also shows good insecticidal activity against Mythimna separate, Helicoverpa armigera, Ostrinia nubilalis, and Spodoptera frugiperda with a death rate of 30%, 25%, 40%, and 25%. Antifungal agent 77 shows toxicity in zebrafish embryo with a LC50 of 2.43 μg/mL[1].
Sulfisoxazole, an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent.Target: Antibacterial; Endothelin ReceptorThe sulfanilamide antibacterial agent sulfisoxazole was found to be a good endothelin receptor antagonist (IC50's of 0.60 microM and 22 microM for the ETA and ETB receptors, respectively) [1]. Sulfisoxazole is used to treat or prevent infections in many different parts of the body. It belongs to the group of medicines known as sulfonamide antibiotics. It works by preventing the growth of bacteria [2].
Ceratotoxin A, a 29-residue peptide isolated from the accessory gland secretion fluid, with strong anti-bacterial activity.
Zanamivir hydrate (5:1) is the hydrate of Zanamivir. Zanamivir is an influenza viral neuraminidase inhibitor with IC50 values of 0.95 nM and 2.7 nM for influenza A and B, respectively[1].
Antibacterial agent 58, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Surfen dihydrochloride is a potent HS (heparan sulfate) antagonist. Surfen binds to glycosaminoglycans. Surfen neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen affects sulfation of heparin and inhibits degradation by heparin lyases. Surfen inhibits FGF2 binding and signaling. Surfen inhibits cell attachment, and virus infection[1].
C18G is a biological active peptide. (C18G is a synthetic α-helical peptide derived from human platelet factor IV. This peptide was found to be antibacterial and is active against Salmonella.)
Bromperidol hydrochloride (R-11333 hydrochloride) possesses antipsychotic activity, with a high affinity for central dopamine receptors D2. Bromperidol hydrochloride can kill mycobacteria in a synergistic manner with Spectinomycin[1][2].
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitory activity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations[1].
Cap-dependent endonuclease-IN-24 is a potent cap-dependent endonuclease (CEN) inhibitor (CN112876510A, DSC1103)[1].
Drosocin is a biological active peptide. (Drosocin is a 19-mer cationic antimicrobial peptide from Drosophila melanogaster. In Drosophila native drosocin carries a disaccharide moiety attached to a threonine residue in mid-chain position. This synthetic drosocin peptide of identical amino acid sequence without the disaccharide has an activity several times lower than the native compound.)
Isoprothiolane-d4 is the deuterium labeled Isoprothiolane. Isoprothiolane is a systemic fungicide. Isoprothiolane is a rice blast controlling agent against the fungal disease of rice planty Pyvioutavia oryzae Cav[1][2].
Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation[1].
Dexamethasone-4,6α,21,21-d4 is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
QPX7728 bis-acetoxy methyl ester is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 42[1].
HF50731 (HF-50731) is a novel potent, selective CXCR4 antagonist with Ki of 19.8 nM in the CXCR4 competitive binding assay.HF50731 significantly inhibited SDF-1α-induced calcium mobilization (IC50=621 nM) and cell migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function (IC50=1.5 uM).The structure-activity relationship analysis demonstrated that HF50731 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288.
Enocitabine, a nucleoside analog, is a potent DNA replication inhibitor and a DNA chain terminator. Enocitabine can be used as an effective chemotherapeutic agent for the treatment of acute myelogenous leukaemia and lymphocytic leukaemias[1].
Antibacterial agent 130 is a 1,1-diarylthiogalactoside, used for targeting the Pseudomonas aeruginosa LecA. Antibacterial agent 130 shows high affinity toward LecA (Kd=1 μM). Antibacterial agent 130 has antibiofilm activity, but lacks bactericidal activity. LecA, a lectin and virulence factor from Pseudomonas aeruginosa involved in bacterial adhesion and biofilm formation[1].
BAL-30072, a siderophore sulfactam, is a monocyclic beta-lactam antibiotic, with activity against multiresistant gram-negative bacilli. BAL30072 shows MIC90 values of 4 μg/mL for MDR Acinetobacter spp. and 8 μg/mL for MDR P. aeruginosa, respectively[1][2].
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
Raxibacumab (ABthrax) is a human IgG1 monoclonal antibody against Bacillus anthracis protective antigen (PA). Raxibacumab blocks the toxin’s deleterious effects by preventing binding of the protective antigen component of the anthrax toxin to its receptors in host cells, thereby blocking the toxin’s deleterious effects. Raxibacumab can be used for anti-anthrax research[1][2].
β-Nor-lapachone is a Candida glabrata antibiofilm agent. β-Nor-lapachone can stimulate ROS production, inhibits efflux activity, adhesion, biofilm formation and the metabolism of mature biofilms of Candida glabrata. β-Nor-lapachone has antifungal activity[1].
MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin[1].
Voriconazole(UK-109496) is a second-generation triazole antifungal used to treat serious fungal infections.IC50 Value: Target: AntifungalVoriconazole displays potent activity against Candida, Cryptococcus and Aspergillus species. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes.
Sotrovimab (VIR 7831) is a human IgG1κ pan-sarbecovirus monoclonal antibody (mAb), neutralizes SARS-CoV-2, SARS-CoV-1, and multiple other sarbecoviruses. Sotrovimab is developed based on S309, exhibits a long half-life and great bioavailability in the respiratory mucosa. Sotrovimab could result in immune-mediated viral clearance and prevent progression of Covid-19 early in the course of disease[1][2].
Propineb (Zinc propylenebis) is a compound widely used in fruit and vegetables cultures, due to its large spectrum of activity against fungal plant diseases[1].
Mupirocin calcium hydrate is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[1][2].
DHFR-IN-10 (compound 4c) is a potent DHFR inhibitor, with an IC50 of 4.21 μM for M. tuberculosis DHFR enzyme. DHFR-IN-10 exhibits potent antituberculosis efficiency[1].