Azidamfenicol is a broad-spectrum chloramphenicol-like antibiotic. Azidamfenicol inhibits ribosomal peptidyltransferase (Ki=22 µM)[1].
Enoxacin is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.Target: antibacterialEnoxacin is a new quinolone carboxylic acid compound. Its activity against 740 bacterial isolates was determined. It inhibited 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml [1]. Daily plasma theophylline concentrations were measured in 14 patients. The mean +/- s.d. theophylline concentrations increased from 8.5 +/- 2.8 micrograms ml-1 prior to enoxacin to a maximum of 21.7 +/- 7.8 micrograms ml-1 during coadministration [2].
Maximin 1 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 1 has cytotoxicity on tumor cells and spermicidal effect[1].
SARS-CoV-2 3CLpro-IN-4 (Compound 5g) is a SARS CoV-2 3CLpro inhibitor with antiviral, antibacterial and antifungal activities[1].
Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis[1][2].
Azidocillin, a semi-synthetic Penicillin, is an orally active β-lactam antibiotic. Azidocillin bears an azide functionality and retains on-target activity within bacteria. Azidocillin can be used to research osteitis caused by dental surgery, otitis media, enterococcal septicemia and other bacterial infectious diseases[1][2][3].
UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide (HY-126373) processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes[1][2].
(+)-(3R,8S)-Falcarindiol is a polyacetylene found in carrots, has antimycobacterial activity, with an IC50 of 6 μM and MIC of 24 μM against Mycobacterium tuberculosis H37Ra[1][2]. Antineoplastic and anti-inflammatory activity[2].
Larcaviximab (c4G7-N) is an IgG1 kappa anti-Ebola virus glycoprotein chimeric monoclonal antibody[1].
Aurachin SS is a nature product that could be isolated from Streptomyces sp. NA04227. Aurachin SS is an antibiotic and has antibacterial activity[1].
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo[1].
ANT3310 sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). ANT3310 sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). ANT3310 sodium can be used in the research of bacterial infection[1][2].
Nemonoxacin (TG-873870) malate is a nonfluorinated quinolone antibiotic. Nemonoxacin malate has broad-spectrum activity against Gram-positive, Gram-negative and atypical pathogens. Nemonoxacin malate can inhibit drug-resistant Streptococcus pneumoniae and (HY-121544) Methicillin-resistant Staphylococcus aureus. Nemonoxacin malate can be used for the research of community-acquired pneumonia[1][2].
SARS-CoV-2-IN-35 is a potent and orally active SARS-CoV-2 M pro inhibitor with a Ki value of 12.1 nM. SARS-CoV-2-IN-35 can be used in research of COVID-19[1].
Tigecycline is a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline dose [3].
Chaetoglobosin C (Compound 4) is a anthraquinone-chromone compound derived from the fungus Chaetomium globosum KMITL-N0802. Chaetoglobosin C has anti-tuberculosis activity [1].
Ebselen is a small-molecule capsid Inhibitor of HIV-1 replication.Target:Ebselen is an organoselenium compound, as an inhibitor of HIV-1 capsid CTD dimerization. Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process. [1] Ebselen is a non-toxic seleno-organic drug with anti-inflammatory and antioxidant properties. Ebselen is an inhibitor of inositol monophosphatase (IMPase). Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. [2]
Psoracorylifol B is a Helicobacter pylori inhibitor with MICs of both 12.5 μg/mL against H. pylori ATCC 43504 and H. pylori SS1[1].
Ertapenem (MK-0826) disodium is a broad spectrum and long acting β-lactam antibiotic. Ertapenem disodium has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem disodium can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract[1][2].
IHVR-17028 is a potent and broad-spectrum antiviral agent. IHVR-17028 exhibits antiviral activity against BVDV, TCRV and DENV with EC50 values of 0.4 μM, 0.26 μM, 0.3 μM, respectively. IHVR-17028 is a potent ER α-glucosidase I inhibitor with an IC50 of 0.24 μM. IHVR-17028 can be used for infectious diseases research[1][2].
Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Antibacterial agent 109 (Compound C-2) is a potent antibacterial agent against both gram-positive and gram negative bacteria, and non-mutagenic. Antibacterial agent 109 inhibits protein synthesis by blocking the extension of new peptide chains[1].
Tioconazole is an antifungal medication.Target: AntifungalTioconazole is an antifungal medication of the Imidazole class used to treat infections caused by a fungus or yeast. Tioconazole topical (skin) preparations are also available for ringworm, jock itch, athlete's foot, and tinea versicolor or "sun fungus". Tioconazole interacts with 14-alpha demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the yeast membrane. In this way, tioconazole inhibits ergosterol synthesis, resulting in increased cellular permeability [1].
Erythromycin-d6 is the deuterium labeled Erythromycin. Erythromycin is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1].
Enrofloxacin hydrochloride is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Tetracycline is a broad-spectrum antibiotic, exhibiting activity against a wide range of gram-positive and gram-negative bacteria.
Rifamycin S is a quinone and an antibiotic agnet against Gram-positive bacteria (including MRSA). Rifamycin S is the oxidized forms of a reversible oxidation-reduction system involving two electrons. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation. Rifamycin S can be used for tuberculosis and leprosy[1][2][3].
Rimonabant-d10 (SR 141716A-d10) hydrochloride is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
Ganciclovir is a potent herpes simplex virus (HSV)inhibitor, including cytomegalovirus (CMV), with an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1).
Chloro-7-deazapurine-β-D-riboside is a nucleoside derivative and has antifungal activity[1].