BO3482 has Antimicrobial activity and can inhibit the growth of methicillin-resistant Staphylococci (MRS) with an MIC90 of 6.25 mg/mL.
Metallo-beta-lactamase ligand 1 is a class B β-lactamase inhibitor with antibacterial activity extracted from patent WO2019221122A1, compound A[1].
Oritavancin diphosphate is a novel semisynthetic glycopeptide antibiotic being developed for the treatment of serious Gram-positive bacterial infections. Target: AntibacterialOritavancin is a lipoglycopeptide.Oritavancin has completed clinical trials and submitted a new drug application for treatment of skin infections.
Sulfachloropyridazine-13C6 is the 13C6 labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
3′-Omethyl-5′-hydroxydiplacone (compound 2), an C-6-geranylflavonoid, can be isolated from the ethanol extract of Paulownia tomentosa fruits. 3′-Omethyl-5′-hydroxydiplacone has antibacterial activity against Gram-positive bacteria[1].
Furagin, nitrofurantoin analog, is an anti-bacterial agent. Furagin is 2-substituted 5-nitrofuran, chemically and structurally similar to well-known antibacterial compound nitrofurantoin.IC50 Value: Target: Antibacterialin vitro: The furagin concentrations in serum remain several hours above the MIC concentrations of many pathogenic bacteria. Despite the high concentrations in serum, the urine levels of furagin were generally lower than those of nitrofurantoin. The 24 hr recoveries in urine were 8--13% for furagin and about 36% for nitrofurantoin [1].in vivo: A time-independent increase in SCE frequency was found in lymphocytes of children treated with furagin. Total CA frequency did not differ significantly between groups of children with various duration of furagin treatment [2]. Women were randomised into two groups receiving either ciprofloxacin 250mg twice a day for 3 days (n=13) or furagin 100mg three times a day for 7 days (n=14). Median lengths of follow-up were 4 days and 5 days in the ciprofloxacin and furagin groups, respectively [3].
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively[1].
BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].
Valnemulin hydrochloride is a pleuromutilin antibiotic which inhibits protein synthesis in bacteria by binding the peptidyl transferase enzyme in the 50s ribosomal subunit.
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra L, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes[1]. Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE[2].
Zabofloxacin (DW-224a Free base) is a novel fluoronaphthyridone quinolone with a 7-pyrrolidone substituent that is considered a potent antibacterial candidate for clinical trials.Zabofloxacin (DW-224a Free base) has excellent activity against gram-positive pathogens including Steptococcus aureus , Streptococcus pyogenes and S.pneumonia.Zabofloxacin (DW-224a Free base) is considered as an alternative candidate for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP)[1].
Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC50 range of 0.1-0.5 μM[1]. Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against S. aureus 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively[2]. Micrococcin P1 is also a potent inhibitor of the malaria parasite Plasmodium falciparum[3].
OX11 is a selective inhibitor of S. pneumoniae, P. aeruginosa, and E. coli bacterial strains[1].
Penetratin-Arg is an antimicrobial and is used for drug delivery vehicle[1].
ThrRS-IN-1 (Compound 30d) is a threonyl-tRNA synthetase (ThrRS) inhibitor with an IC50 of 1.4 µM and a Kd of 1.36 µM against Salmonella enterica ThrRS (SeThrRS). ThrRS-IN-1 simultaneously targets the tRNAThr and L-threonine binding pockets of ThrRS. ThrRS-IN-1 shows potent antibacterial activities[1].
NOSO-502 (NOSO502) is a novel inhibitor of bacterial translation, has MIC values of 0.5-4 ug/ml against standard Enterobacteriaceae strains and carbapenem-resistant Enterobacteriaceae (CRE) isolates that produce KPC, AmpC, or OXA enzymes and metallo-β-lactamases; interacts strongly with a specific site on the 30S subunit of bacterial ribosomes but has no significant activity against any of the 55 cell surface receptors, transporters, or ion channels; NOSO-502 is active against a panel of Gram-positive and Gram-negative bacteria, including carbapenem-resistant and polymyxin-resistant strains, and exhibits promising in vivo activity in various murine infection models, a favorable in vitro safety profile, and a low potential for resistance development.
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity[1][2].
1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone is a potent antibacterial agent with an MIC50 value of 22 µM and an MIC90 value of 50 µM for Helicobacter pyloriStrain 51. 1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone has the potential for the research of gastric and duodenal ulcers[1].
Polyphemusin I is a natural antimicrobial peptide with excellent antimicrobial activity against Gram-negative and Gram-positive bacteria. Polyphemusin I contains 18 amino acids and is stabilized into an amphiphilic, antiparallel β-hairpin by two disulfide bridges[1].
TH-Z145, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 210 nM)[1].
Antitubercular agent-14 (Compound 1) is an antitubercular agent with an MIC of 0.3 µg/mL against M. tuberculosis[1].
Omodenbamab is an anti-SpA (Staphylococcal protein A) humanized monoclonal antibody with a KD value of 0.0467 nM. Omodenbamab circumvents a key S. aureus evasion mechanism by targeting the cell wall moiety Protein A (SpA). Omodenbamab can be used in research of S. aureus bloodstream infection[1].
Loracarbef-d5 is the deuterium labeled Loracarbef. Loracarbef, a cephalosporin antibiotic, is an orally active second-generation synthetic beta-lactam antibiotic of the carbacephem class[1][2].
Hexahydrohippuric acid is a metabolite of Shikimate acid in both liver and kidney, under microbial metabolism effect. Hexahydrohippuric acid is made of cyclohexane carboxylic acid and glycinamide, and shows antibacterial activity[1][2].
Transtorine is a quinoline alkaloid, found from Ephedra transitoria, with antibacterial activity[1].
Allicin (diallyl thiosulfinate), a highly potent natural antimicrobial activity substance, inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains[1].
Pikromycin is a macrolide antibiotic that has been found in S. venezuelae and active against E. coli, S. aureus and B. subtilis[1].
Macrocarpal D is a potent antibacterial agent. Macrocarpal D is a phloroglucinol dialdehyde diterpene derivatives that can be found in the leaves of Eucalyptus macrocarpa[1].
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive[1][2].
Sutezolid (PNU-100480) is an oxazolidinone antimicrobial being developed for the treatment of tuberculosis.Target: AntibacterialSutezolid is a much-awaited drug candidate for treatment of Mycobacterium tuberculosis. [1] Sutezolid is an oxazolidinone antibiotic currently in development as a treatment forextensively drug-resistant tuberculosis. Sutezolid is a linezolid analog with superior bactericidal activity against Mycobacterium tuberculosis in the hollow fiber, whole blood and mouse models. Like linezolid, it is unaffected by mutations conferring resistance to standard TB drugs. This study of sutezolid is its first in tuberculosis patients.[2]