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].
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].
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].
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].
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].
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].
Ombuoside is a glycoside ombuoside isolated from Gynostemma pentaphyllum.Ombuoside has antimicrobial activity against several strains of gram-positive and gram-negative bacteria and the yeast Candida albicans[1]. Ombuoside has antioxidant effects by scavenging free radicals and ROS[2].
Vulpinic acid, a lichen metabolite, decreases H2O2-induced ROS production, oxidative stress and oxidative stress-related damages in human umbilical vein endothelial cells (HUVEC). Vulpinic acid is active against staphylococci, enterococci, and anaerobic bacteria.Vulpinic acid has the potential for atherosclerosis research[1][2].
14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities[1].
Ianthelliformisamine B diTFA is a bromotyrosine-derived antibacterial agent. Ianthelliformisamine B diTFA is against E. coli and S. aureus strains with MICs of 14.5 μM and 144.7 μM[1].
Ozenoxacin is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
DU011 is a noncanonical anti-infective agent and small-molecule inhibitor of capsule biogenesis, targets MprA (Kd=30 nM), a MarR family transcriptional repressor of multidrug efflux pumps, inhibits capsule expression in E. coli.DU011 does not alter Escherichia coli antibiotic resistance and has significantly enhanced inhibition of capsule expression, compared with other proposed MprA ligands, such as salicylate and 2,4-dinitrophenol (DNP).
Patchouli alcohol is a natural tricyclic sesquiterpene extracted from Pogostemon cablin (Blanco) Benth, and exhibits anti-Helicobacter pylori and anti-inflammatory properties[1].
Bleomycin sulfate is a DNA synthesis inhibitor with potent antitumor activity.