pneumoniae

Chlamydia pneumoniae-IN-1 is a benzimidazole analog that inhibits Chlamydia pneumoniae at low concentrations.Chlamydia pneumoniae-IN-1 exhibits antimicrobial activity with a MIC of 12.6 μM against CV-6 strains, and can be used for the study of pulmonary infections.Chlamydia pneumoniae-IN-1 is a benzimidazole analog that inhibits Chlamydia pneumoniae at low concentrations.Chlamydia pneumoniae-IN-1 has been used in the study of pulmonary infections.

6'-hydroxydihydrocinchonidine is a metabolite of quinine, with antimicrobial and antitumor activity, and inhibitory effect on Trypanosoma brucei and Streptococcus pneumoniae.

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates. It exhibits inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg/ml, 4 μg/ml, and 16 μg/ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

LpxH-IN-AZ1 is a potent inhibitor of the UDP-2,3-diacylglucosamine pyrophosphate hydrolase, LpxH, and sulfonylpiperazine compounds.LpxH-IN-AZ1 exhibits antimicrobial activity and inhibits Klebsiella pneumoniae with an IC50 of 0.36 μM.

α-(difluoromethyl)-DL-Arginine (RMI 71897) is an enzyma-activated, irreversible inhibitor of arginine decarboxylase for E. coli (Ki = 800 μM), Pseudomonas aeruginosa, and Klebsiella pneumoniae. At 0.01 mM, it has been shown to prevent osmotic stress-induced increases in arginine decarboxylase activity and putrescine synthesis in oat leaf cells. When combined with a variety of polyamine analogues, α-(difluoromethyl)-DL-Arginine inhibited the growth of Trypanosoma Crui in mammalian host cells at a minimum concentration of 10 mM and prevented the growth of Trypanosoma Crui in T-cell receptor alpha-deficient mouse models.

Delafloxacin (WQ-3034) (RX-3341, ABT-492) is a fluoroquinolone antibiotic agent. It has potent inhibitory against levofloxacin-resistant Streptococcus pneumoniae strains (MIC: 0.0078-0.125 μg/ml).

Moxifloxacin (Avelox) is a fourth-generation fluoroquinolone that has been shown to be effective against Gram-positive, Gram-negative, and atypical strains, as well as multi-drug resistant Streptococcus pneumoniae.

CSP1 is a highly potent and selective agonist of the ComD1 receptor, exhibiting an IC50 value of 10.3 nM. It represents a major variant of competence-stimulating peptide (CSP) and plays a crucial role in regulating the genetic transformation of S. pneumoniae through modulation of quorum sensing (QS). Additionally, CSP1 possesses antibacterial activity, further enhancing its potential as an effective antibacterial agent.

Ceftaroline fosamil hydrate acetate is a powerful cephalosporin antibiotic that exhibits broad-spectrum efficacy against both Gram-positive pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative bacteria. It possesses anti-infective properties suitable for studying complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP) [1] [2] [3].

CHEMBL1276927 (N-(3-(1H-benzo[d]imidazol-2-yl)phenyl)-3-methylbenzamide) shows antibacterial and antiparasitic activities against Chlamydia pneumoniae and Leishmania donovani.

Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg/ml, respectively.References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984). Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin .1 Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus with MIC values of 120, 24, 34, and 0.42 μg/ml, respectively. References1. Jones, R.N., and Packer, R.R. Cefotaxime, cephalothin, and cephapirin: Antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations. Diagn. Microbiol. Infect. Dis. 2(1), 65-68 (1984).

MurF-IN-1 (Compound 7) is an inhibitor of the MurF enzyme, exhibiting an inhibitory concentration with a pIC50 value of 5.19 in assays targeting Streptococcus pneumoniae MurF [1].

Actinopyrone A is a pyrone isolated from S. pactum with diverse biological activities. It has selective and potent antimicrobial activity against H. pylori (MIC = 0.1 ng/mL) with no activity against other Gram-negative bacteria including E. coli, K. pneumoniae, P. aeruginosa, and B. fragilis. Actinopyrone A also mildly inhibits growth of Gram-positive bacteria and dermatophytes with MIC values ranging from <6.25 to 25 μg/mL. Intravenous administration of actinopyrone A (30 μg/kg) increases coronary blood flow in dogs by 196.2%.

Nybomycin is a fungal metabolite originally isolated from Streptomyces sp. A717 and has antibacterial activity. It is active against B. subtilis, B. cereus, B. mycoides, M. smegmatis, and K. pneumoniae (MICs = 0.025, 2, 0.8, 0.2, and 0.003 μg/ml, respectively). Nybomycin is also active against M. tuberculosis and M. bovis (MICs = 4.5 and 1 μg/ml, respectively).

Desotamide is a cyclic hexapeptide antibiotic originally isolated from Streptomyces. It is active against S. aureus, S. pneumoniae, and methicillin-resistant S. epidermidis (MRSE; MICs = 16, 12.5, and 32 μg/ml, respectively).

Colistin (Polymyxin E), a polypeptide antibiotic with oral activity, exhibits strong efficacy against a range of Gram-negative rod-shaped bacteria, such as multidrug-resistant Pseudomonas aeruginosa, Acinetobacter baumannii, and Klebsiella pneumoniae. However, its use is associated with nephrotoxicity. It is primarily utilized in researching infections caused by Gram-negative bacilli [1] [2].

Poly(I:C):Kanamycin (1:1) sodium is a symmetric complex combining Poly(I:C) sodium, a synthetic double-stranded RNA analog acting as a TLR3 and RIG-I/MDA5 agonist, with Kanamycin, an antibacterial agent effective against both Gram-negative and positive bacteria by inhibiting translocation and causing miscoding on the 70S ribosomal subunit. Poly(I:C) sodium serves as a potent vaccine adjuvant, bolstering innate and adaptive immunity and prompting apoptosis in cancer cells [1] [2]. Meanwhile, Kanamycin exhibits significant efficacy against Mycobacterium tuberculosis, including drug-resistant strains, and Klebsiella pneumoniae, offering valuable insights for tuberculosis and pneumonia research [3] [4] [5] [6].

Rifalazil is a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis (MIC: 0.00025 to 0.0025 μg/ml).

Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)

Competence-Stimulating Peptide-2 (CSP-2) is a quorum sensing signal peptide synthesized by Streptococcus pneumoniae. ComD2, a compatible receptor of CSP-2, exhibits an EC 50 value of 50.7 nM.

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg/ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, flumequine (50 mg/kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

2,3,8-tri-O-Methyl ellagic acid has antimicrobial activity agaist Vibro cholera, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacillus cereus, Escherichia coli.

(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MICs = 0.16-0.21 μg/ml). It inhibits polymerization and the GTPase activity of E. coli FtsZ, a tubulin-like GTPase involved in bacterial cell division (IC50s = 8.2 and 7 μg/ml, respectively). (-)-Viriditoxin inhibits proliferation of human DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5.36, 0.63, and 7.6 μM, respectively) . It is also toxic to mice (LD50 = 2.8 mg/kg, i.p.).

DNA gyrase B-IN-2 (Compound E), a 2-aminobenzothiazole derivative, serves as a potent inhibitor of DNA gyrase B with substantial efficacy against ESKAPE pathogens. The compound exhibits potent nanomolar-range inhibition (IC 50 < 10 nM) and a broad-spectrum antibacterial effect, with minimum inhibitory concentrations below 0.03 μg/mL for most Gram-positive species and between 4–16 μg/mL for Gram-negative species including E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae. DNA gyrase B-IN-2 is applicable in infection research [1].

Leucomycin a5 is a metabolite from the leucomycin complex, which was originally isolated from S. kitasatoensis. It is active against a variety of Gram-positive and Gram-negative bacteria (MICs = 0.04-0.8 µg/ml) but not against K. pneumoniae, S. typhimuriu

Murraol shows the significant proliferative activities on osteoblast-like UMR106 cells lines at the concentration of 1 × 10-10 mol/L. It and auraptenol show 63 ug/mL MIC value against Klebsiella pneumoniae ATCC 4352 and Bacillus subtilis ATCC 9372.

10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).

Neocyclomorusin displays minimal inhibitory concentration (MIC) value of 4 ug/mL against Klebsiella pneumoniae ATCC11296, Enterobacter cloacae BM47.

TP0586532 is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg/ml, respectively). It is cytotoxic to B16/F10 and Moser cells (IC50s = 0.0008 and 0.04 μg/ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

Obafluorin is a β-lactone antibiotic that has been found in P. fluorescens.1 It is active against S. aureus, S. faecalis, K. pneumoniae, and P. vulgaris (MIC = 125 μg/ml for all). |1. Pu, Y., Lowe, C., Sailer, M., et al. Synthesis, stability, and antimicrobial activity of (+)-obafluorin and related β-lactone antibiotics. J. Org. Chem. 59(13), 3642-3655 (1994).

Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg/ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg/g in the diet. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is a defensin mimetic antibiotic compound, exhibiting potent anti-infective antimicrobial activity against a range of bacteria. It demonstrates MIC90 values of 1 μg/mL and 8 μg/mL against the Gram-positive bacteria Streptococcus pneumoniae and Streptococcus viridans, respectively. Additionally, it has a MIC90 value of 8 μg/mL for the Gram-negative bacteria Haemophilus influenzae and a MIC90 value of 4 μg/mL for Pseudomonas aeruginosa.

Omadacycline is an aminomethylcycline antibiotic. Omadacycline demonstrated net cidal activity in relation to the initial burden against four strains of Streptococcus pneumoniae.

Cefazolin-13C2,15N is intended for use as an internal standard for the quantification of cefazolin by GC- or LC-MS. Cefazolin is a broad-spectrum cephalosporin antibiotic that is active in vitro against various Gram-positive and Gram-negative bacteria (MICs = 0.2-12.5 μg/ml). It also inhibits the growth of clinical isolates of S. aureus, E. coli, P. mirabilis, and K. pneumoniae (MICs = 0.1-25 μg/ml). In vivo, cefazolin protects against S. aureus, E. coli, and P. mirabilis infection in mice (ED50s = <0.09-1.78, 0.44-3.63, and 2.31-5.2 mg/animal, respectively). Formulations containing cefazolin have been used to treat a variety of bacterial infections.

OM173-αA is a quinone bacterial metabolite that inhibits the growth of the bacteria M. gallisepticum, M. pneumoniae, and S. aureus. OM173-αA also inhibits the growth of the plant pathogenic fungus P. oryzae and several species of Trichophyton.

Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a derivative of quinine with antimicrobial activity against Streptococcus pneumoniae.Ethylhydrocupreine hydrochloride has antimalarial activity with an IC50 of 25.75 nM for Plasmodium falciparum. Ethylhydrocupreine hydrochloride has antimalarial activity with an IC50 of 25.75 nM against Plasmodium falciparum.Ethylhydrocupreine hydrochloride is an agonist of Gallus gallus2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7).

TP0586352 is a potent inhibitor of LpxC, exhibiting efficacy against carbapenem-resistant strains of Klebsiella pneumoniae without inducing cardiovascular risks.

DS86760016 is a highly effective inhibitor of leucyl-tRNA synthetase (LeuRS), demonstrating potent activity against multidrug-resistant (MDR) Gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Notably, DS86760016 effectively inhibits LeuRS enzymes derived from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, exhibiting IC50 values of 0.38 μM, 0.62 μM, and 0.16 μM, respectively.

(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g/ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g/ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg/ml, respectively).1 1.Sassa, T., and Igarashi, M.Structures of (-)-mycousnine, (+)-isomycousnine and (+)-oxymycousnine, new usnic acid derivatives from phytopathogenic Mycosphaerella nawaeAgric. BioI. Chem.54(9)2231-2237(1990) 2.Lee, J., Lee, J., Kim, G.J., et al.Mycousfurans A and B, antibacterial usnic acid congeners from the fungus Mycosphaerella sp., isolated from a marine sedimentMar. Drugs17(7)422(2019)

KPC-2-IN-2 (Compound 6c) is a potent Klebsiella pneumoniae carbapenemase (KPC-2) inhibitor with Ki of 0.038 μM. KPC-2-IN-2 can enhance the activity of cefotaxime in E. coli expressing KPC-2 [1].

Solithromycin (OP-1068) is an orally bioavailable antimicrobial agent that inhibits cell viability, protein synthesis, and growth rate of Streptococcus pneumoniae, Staphylococcus aureus, Staphylococcus aureus, and Haemophilus influenzae with IC50 values of 7.5 ng/mL, 40 ng/mL, and 125 ng/mL, respectively.Solithromycin inhibits protein biosynthesis by binding to the large 50S subunit of the ribosome.

P1 is a broad-spectrum antimicrobial peptide exhibiting antibacterial activity against both Gram-positive and Gram-negative bacteria, including B. anthracis spores and Carbapenem-resistant strains of A. baumannii and K. pneumoniae [1].

4-Trehalosamine, a microbial metabolite identified in Streptomyces, exhibits antibiotic properties. Demonstrating efficacy in cup assays, it is active against E. coli, K. pneumoniae, and B. subtilis at concentrations of 0.5, 1, and 2 mg/ml.

Polymyxin B2, a significant component of polymyxin B, is an antibiotic cationic lipopeptide initially derived from B. polymyxa. This compound effectively inhibits P. aeruginosa, A. baumannii, K. pneumoniae, and E. cloacae strains, exhibiting minimum inhibitory concentrations (MICs) of 1-2, 0.5-1, 0.25-0.5, and 0.25-1 µg/ml, respectively. Notably, in a mouse model of P. aeruginosa bloodstream infection, administration of polymyxin B2 at a dosage of 4 mg/kg has been shown to decrease the number of colony-forming units (CFUs) in the blood.

(±)-ε-Viniferin, a racemate of ε-Viniferin, exhibits P450 inhibitory antioxidants, along with hepato-protective and antimicrobial activities. It also demonstrates antibacterial and antibiofilm activities against Gram-positive bacteria Streptococcus pneumoniae, with a minimum inhibitory concentration (MIC) of 20 μM [1].

3-Bromotyrosine, a product of protein oxidation, is generated after eosinophil activation during allergic responses. It serves as a biomarker for eosinophil peroxidase-induced protein oxidation both in vitro and in vivo. Beyond its association with eosinophils, 3-bromotyrosine levels are significantly elevated in peritoneal exudate from K. pneumoniae-infected mice, indicating a fivefold increase compared to uninfected controls, which implies that neutrophils may release increased levels of oxidized products during inflammation. Furthermore, in humans, allergen-challenged lung samples from patients with allergen-induced asthma show a tenfold increase in 3-bromotyrosine, highlighting its potential as a marker for oxidative stress in allergic conditions.

Doripenem is a broad-spectrum carbapenem antibiotic effective against both Gram-negative and Gram-positive bacteria, such as S. aureus, S. pneumoniae, E. coli, and K. pneumoniae, with minimum inhibitory concentrations (MICs) ranging from less than 0.015 to 0.3 µg/ml. It has been proven to reduce the viable bacteria count in mouse lung models of chronic P. aeruginosa respiratory tract infection at a dosage of 100 mg/kg per day. Doripenem operates by inhibiting bacterial cell wall synthesis through the formation of stable acyl-enzyme complexes with penicillin-binding proteins, leading to their inactivation. This compound has been utilized in various formulations for the treatment of bacterial infections.

Faropenem daloxate (Faropenem medoxil) is useful for penem and antibiotics. Faropenem medoxomil has excellent in vitro activity against Streptococcus pneumoniae, Haemophilus influenzae and other key pathogens implicated in acute bacterial rhinosinusitis.Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.

CAP 3 is a cholic acid-peptide conjugate (CAP) with antibacterial activity. It is active against the Gram-negative bacteria E. coli, K. pneumoniae, and A. baumanii (MIC99s = 8, 16, and 16 μM, respectively). CAP 3 increases the fluidity of model Gram-negative bacterial membranes and binds to LPS in vitro. It reduces the biomass and number of colony-forming units in E. coli biofilms in a concentration-dependent manner. CAP 3 inhibits E. coli biofilm formation on catheters implanted in mice infected with E. coli at the incision site when applied as a coating on the catheters. CAP 3 (40 mg/kg) also reduces bacterial load in E. coli-infected wounds in mice. It is cytotoxic to A459 cells (IC50 = 56.4 μM) and has hemolytic activity against human red blood cells with a 50% lysis (HC50) value of 48 μM.