Antibacterial agent 35, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in treating both Gram-positive and Gram-negative bacterial infections in mice[1][2].
Methacycline HCl is a tetracycline antibiotic.Target: Antibacterial Methacycline HCl is a broad-spectrum semisynthetic antibiotic related to tetracycline but excreted more slowly and maintaining effective blood levels for a more extended period.
Antitubercular agent-9 shows effective antitubercular activity with a MIC value of 1.03-2.32 μM.
Capreomycin is a peptide antibiotic, commonly grouped with the aminoglycosides, which is given in combination with other antibiotics for MDR-tuberculosis.IC50 value:Target: The drug should not be given with streptomycin or other drugs that may damage the auditory vestibular nerve. Patients on this drug will often require audiology tests. It is a cyclic peptide.Capreomycin is administered intramuscularly and shows bacteriostatic activity.
Sarafloxacin hydrochloride is a quinolone antibiotic drug.Target: Antibacterialsarafloxacin hydrochloride is a fluoroquinolone antibiotic registered for use against poultry diseases. Sarafloxacin treatment demonstrated mineralization to 14CO2 amounting to 0.58%, 0.49%, and 0.57% in loam, silt loam, and sandy loam soils, respectively, at the termination of the test [1]. The inhibitory level of sarafloxacin for the tested bacteria was strain dependent. It appeared that in broth culture Escherichia coli isolates were sensitive to sarafloxacin concentrations 5-fold lower than the concentrations present in the simulated gut model, suggesting that sarafloxacin may be partially unavailable due to absorption to organic matter in the model [2]. Administering Sarafloxacin hydrochloride in the feed for 5 d at a dose of 10 or 12.5 mg/kg of fish proved efficacious in treating channel catfish infected with E. ictaluri in all three field trials. Average survival of the nonmedicated group was 43% in trial 1, 11°% in trial 2, and 59% in trial 3. Survival of the corresponding Sarafloxacin hydrochloride-medicated groups averaged 68, 48, and 73%. Antibiotic therapy with Sarafloxacin hydrochloride significantly (P < 0.05) improved survival in all trials [3].
Antibacterial agent 41 (example 3) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Ethionamide(2-ethylthioisonicotinamide) is an antibiotic used in the treatment of tuberculosis.Target: AntibacterialEthionamide is a second-line antitubercular agent that inhibits mycolic acid synthesis. It also may be used for treatment of leprosy. Ethionamide is a prodrug. It is activated by the enzyme EthA, a mono-oxygenase in Mycobacterium tuberculosis, and binds NAD+ to form an adduct which inhibits InhA in the same way as isoniazid. Expression of the ethA gene is controlled by EthR, a transcriptional repressor. It is understood that improving ethA expression will increase the efficacy of ethionamide and so EthR inhibitors are of great interest to co-drug developers. The action may be through disruption of mycolic acid [1, 2].
cOB1 phermone, a bacterial sex pheromone, effectively inhibits multidrug-resistant Enterococcus faecalis V583[1].
Marbofloxacin hydrochloride is a potent antibiotic of which depends upon its inhibition of DNA-gyrase.Target: DNA-gyraseMarbofloxacin hydrochloride is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin hydrochloride is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].Administration of Marbofloxacin hydrochloride at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin hydrochloride were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin hydrochloride was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin hydrochloride absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin hydrochloride dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3]. Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Ampicillin is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
Protein kinase G inhibitor-1 (Compound 270) is a mycobacterial protein kinase G inhibitor, with an IC50 of 0.9 μM. Protein kinase G inhibitor-1 can be used for mycobacterial infection research[1].
Afabicin is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase[1]. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml[3]. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB)[2].
GSK656 is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.
Papyracillic acid, a fungal metabolite, a Penicillic acid analog, is a nonselective herbicide. Papyracillic acid has anti-bacterial, anti-fungal, nematicidal, and phytotoxic effects[1].
Propylparaben sodium is an antimicrobial agent, preservative, flavouring agent[1].
Pralurbactam is a β-Lactamase inhibitor. Pralurbactam can be used for research of bacterial infection[1][2].
Meropenem is a carbapenem antibiotic, which displaying a broad spectrum of antibacterial activity.Target: AntibacterialMeropenem, a new parenteral carbapenem demonstrated increased activity as compared to imipenem against 336 strains of Neisseria gonorrhoeae, 119 strains of Haemophilus influenzae, and 110 strains of H. Ceftriaxone and ciprofloxacin demonstrated activity superior to that of both carbapenems while the activity of ceftazidime was similar to that of meropenem [1]. Meropenem, like imipenem and various experimental penems, may overcome the resistance problems presented by Class I beta-lactamases [2]. MEROPENEM was rapidly penetrated to the pleural effusion and was retained for a more prolonged time in the pleural effusion than in the blood of patients with accumulated pleural effusion, and it suggested the usefulness of MEROPENEM in antibacterial therapy for patients with pleurisy causing accumulation of pleural effusion [3].Clinical indications: Appendicitis; Bacterial infection; Bacterial meningitis; Bacterial pneumonia; Bacterial respiratory tract infection; Bacterial skin infection; Bacterial urinary tract infection; Bacteroides fragilis infection; Bacteroides infection; Bacteroides thetaiotaomicron infection; Complicated skin and skin structure infectionFDA Approved Date: July 1996Toxicity: In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Nanchangmycin, produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
Peptide 5g is an antimicrobial peptide. Peptide 5g inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 10, 12.5 μg/mL respectively[1].
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor, with IC50 values of 0.1 μM (VIM-1), 1.3 μM (NDM-1), and 5.0 μM (IMP-7), respectively[1].
Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K+ efflux and inhibits cell viability with EC50 of 5 μM[1].
Clindamycin is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla)[1].
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
Chloramphenicol is a broad-spectrum antibiotic.Target: AntibacterialChloramphenicol is a bacteriostatic drug that stops bacterial growth by inhibiting protein synthesis. Chloramphenicol prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome. It specifically binds to A2451 and A2452 residues in the 23S rRNA of the 50S ribosomal subunit, preventing peptide bond formation. While chloramphenicol and the macrolide class of antibiotics both interact with ribosomes, chloramphenicol is not a macrolide. It directly interferes with substrate binding, whereas macrolides sterically block the progression of the growing peptide [1, 2].
Cetalkonium chloride is an ammonium antiseptic agent used in many topical drugs for infections of mouth, throat and eye. Cetalkonium chloride acts as anti-inflammatory amphiphilic agent[1].
G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity[1].
Antibacterial agent 143 (Compound 5a) is an antibacterial agent with MICs of 25, 25, 50 and 50 μg/mL against B. subtilis ATCC6633, . aureus ATCC6538, P. aeruginosa ATCC13525 and E. coli ATCC35218, respectively[1].