Phleomycin is a wide-spectrum glycopeptide antibiotic found in Streptomyces verticillus. Phleomycin, an effective DNA-cleaving agent, binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A)[1].
Cyproconazole is a triazole fungicide that is used agriculturally for protection of crops against a wide variety of fungal pathogens.In vitro: Cyproconazole has been shown to cause a dose dependent inhibition of progesterone production in human placental cells in vitro. cyproconazole exhibited the lowest capacity to increase CYP1A1 and were not able to activate the AhR in the transactivation assay. [1]In vivo: Cyproconazole, a triazole fungicide, causes hepatocellular adenomas and carcinomas in CD-1 mice at dose levels of 100 and 200 ppm. In wild-type mice, 200 ppm cyproconazole caused liver hypertrophy, increased liver weight and cell proliferation, single-cell necrosis and fat vacuolation. [2]
Antibacterial agent 55 (example 21) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Urease-IN-3 (Compound L12) is a potent inhibitor of Urease with an IC50 of 1.449 μM. Urease-IN-3 is a flavonoid analogue compound[1].
Antistaphylococcal agent 2 is an antistaphylococcal therapeutic agent.
Anti-inflammatory agent 14 (compound 28) is an anti-inflammatory agent, with a MIC50 of 2 μM for Mtb H37Rv[1].
Curzerenone is one of constituents of leaf essential oil extracted from L. pulcherrima. Shows slight inhibitory effective against E. coli[1].
Ceftaroline fosamil (TAK-599) inner salt, a cephalosporin derivative, is an N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil inner salt can be used for the research of MRSA infection[1][2][3].
Acetylspiramycin is a macrolide antibiotic.
Monolaurin (1-Monolaurin) possesses anti-viral and anti-bacterial activity[1][2].
Cefonicid sodium is a broadspectrum cephalosporin antibiotic which inhibits the formation of the bacterial cell wall. Target: AntibacterialCefonicid sodium can inhibit the carnitine/carnitine antiport when it is added internally and externally to proteoliposomes. It is known that the molecule contains various electroactive groups that can be detected using adsorptive square-wave stripping voltammetry. In addition, the compound can be detected in solution using UV spectroscopy at 265 nm. Cefonicid sodium is effective against Escherichia coli, Klebsiella, Citrobacter, Enterobacter, indole-negative Proteus, and Providencia.
ARC7 can act as a probe for secondary metabolism in S. coelicolor. ARC7 is a tool for studying secondary metabolism and the streptomycete life cycle[1].
Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF)[1].
Pipecolic acid-d9 is the deuterium labeled Pipecolic acid. Pipecolic acid, a metabolite of Lysine, is an important precursor of many useful microbial secondary metabolites. Pipecolic acid can be used as a diagnostic marker of Pyridoxine-dependent epilepsy[1][2].
Tigecycline mesylate a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline mesylate 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 mesylate 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 mesylate 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 mesylate appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline mesylate 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 mesylate 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 mesylate dose [3].Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infectionFDA Approved Date: June 17, 2005 Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
Cefradine is a first generation cephalosporin antibiotic.
Cefmetazole sodium is a semisynthetic cephamycin antibiotic. Target: AntibacterialCefmetazole sodium has a broad spectrum of activity comparable to that of the second-generation cephalosporins, covering gram-positive, gram-negative, and anaerobic bacteria. Unlike the second-generation cephalosporins, cephamycins such as cefmetazole are usually active against Bacteroides fragilis. Cefmetazole is also active against beta-lactamase-producing organisms that are resistant to first-generation cephalosporins or penicillins. The pharmacokinetics of cefmetazole allow parenteral administration (intravenous or intramuscular) 2-3 times daily for treatment of infection. The drug has been studied in gynecologic, intraabdominal, urinary tract, respiratory tract, and skin and soft tissue infections. Administered preoperatively, it may reduce the frequency of infection in certain clean-contaminated or potentially contaminated procedures, including cesarean section, abdominal or vaginal hysterectomy, cholecystectomy (high-risk patients), and colorectal surgery.
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6[1].(Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) [2].
Tylvalosin tartrate (Acetylisovaleryltylosin tartrate) is a macrolide antibiotic that can against Gram-positive bacteria[1][2].
Rhein-8-glucoside calcium, an anthraquinone compound, is isolated from the EtOH extract of the roots of Saussurea lappa. Rhein-8-glucoside calcium is an hPTP1B inhibitor, with an IC50 of 11.5 μM. Rhein-8-glucoside calcium has antibacterial effects[1][2].
Antibacterial agent 37 is an antibacterial agent extracted from patent WO2015063714A1, compound B. Antibacterial agent 37 can be used for the research of bacterial infections[1].
Indolmycin (TAK-083), an antibiotic, is a competitive inhibitor of prokaryotic tryptophanyl-tRNA ligase (TrpS). Indolmycin (TAK-083) possesses both anti-viral and anti-bacterial activity[1][2][3].
β-Pinene ((-)-β-Pinene), a major component of turpentine, inhibit infectious bronchitis virus (IBV) with an IC50 of 1.32 mM. β-Pinene presents antimicrobial activity[1][2].
Antitubercular agent-28 (compound 2) is a potent antitubercular agent with an IC50 value of 1.5 µM, an MIC value of 4.5 µM, an IC90 value of 2.5 µM. Antitubercular agent-28 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity[1].
(Rac)-Fosfomycin (benzylamine)-13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
Carumonam (AMA-1080; Ro 17-2301) is a sulfonated monocyclic β-Lactam Antibiotic, targeting to penicillin-binding protein (PBP). Carumonam exerts highly activity against Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae, while it weakly and even inactively inhibits Streptococcus pneumoniae and Staphylococcus aureus. Carumonam is resistant to beta-lactamase-mediated hydrolysis[1].
Oxacillin sodium salt is a narrow-spectrum β-lactam antibiotic of the penicillin class.
Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties[1].
DL-Histidine-15N is a 15N-labeled Pefloxacin.
PF-04753299 is a potent and selective UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitor. PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection[1].