pneumoniae

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

Chlamydia pneumoniae-IN-1 (compound 55), a benzimidazole derivative, exhibits potent antibacterial activity, inhibiting 99% of C. pneumoniae growth at a concentration of 10 μM while maintaining 95% viability of host cells. It effectively inhibits the CV-6 strain of C. pneumoniae with a minimum inhibitory concentration (MIC) of 12.6 μM, demonstrating its antichlamydial efficacy [1].

Lipopolysaccharides from Klebsiella pneumoniae (LPS, from bacterial [Klebsiella pneumoniae]) are lipid-polysaccharide endotoxins and TLR4 activators originating from Klebsiella pneumoniae, classified as S-type LPS. They exhibit a characteristic tripartite structure comprising an O-antigen, a core oligosaccharide, and lipid A. These lipopolysaccharides may contribute to bacterial immune evasion by inhibiting complement-mediated killing and suppressing host antimicrobial peptide secretion, thus helping bacteria evade immune defenses. Possessing high viscosity and serum resistance, they can potentially induce sepsis. Additionally, these lipopolysaccharides are utilized in the development of animal models for sepsis/septicemia.

Blasticidin S HCl is a natural product and an inhibitor of protein synthesis. Blasticidin S HCl is a broad-spectrum antibiotic that can inhibit the cell growth of prokaryotes, fungi, plants and mammalian cells.

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.

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 and exhibiting 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].

Meropenem (SM 7338) is a broad-spectrum carbapenem antibiotic administered intravenously for severe bacterial infections caused by sensitive agents. It commonly causes mild, transient aminotransferase elevations and can rarely lead to clinically apparent cholestatic liver injury.

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.

3,5-Dimethylbenzaldehyde has broad-spectrum antimicrobial activity, inhibiting Bacillus subtilis, Pseudomonas albicans, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus pneumoniae.

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).

Copper(Ⅱ) Sulfate (Cupric sulfate) has a variety of antibacterial activities and has inhibitory activity against Staphylococcus aureus, Streptococcus pneumoniae, Pseudomonas aeruginosa, Plasmodium falciparum, etc.

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

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.

JH-LPH-33 is a UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH inhibitor with antimicrobial activity for the study of bacterial infections.

Cefditoren is an antibiotic characterized by its oral efficacy and broad-spectrum antimicrobial activities, effectively inhibiting both Gram-negative and Gram-positive bacterial activities. It displays a MIC50 of 0.25-0.5 mg/L against Streptococcus pneumoniae strains. Additionally, Cefditoren is utilized in treating respiratory and skin infections.

Nafithromycin (WCK 4873) serves as an orally administered antibiotic effective against community-acquired pneumonia organisms such as Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, and Methicillin-susceptible Staphylococcus aureus. It displays a minimum inhibitory concentration (MIC 90) of 0.12 mg/liter against both macrolide-resistant and telithromycin-insensitive Streptococcus pneumoniae.

RNAP-NusG-IN-1 is an inhibitor of RNAP-NusG. It exhibits antibacterial (bacterial) activity against Gram-positive bacteria, with the most potent effect observed in Streptococcus pneumoniae, where the minimum inhibitory concentration (MIC) is 1 μg/mL.

MLEB-22043 is a synthetic siderophore-monocyclic β-lactam conjugate which enters bacteria through TonB-dependent transport proteins utilizing its siderophore component, subsequently exerting antibacterial activity via its β-lactam portion. This compound acts as a broad-spectrum antibiotic, exhibiting significant inhibitory activity against pathogens such as Klebsiella pneumoniae, Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa.

Debio-1452-NH3 is a novel and potent FabI antibody—enoyl-acyl carrier protein reductase inhibitor that demonstrates excellent efficacy in reducing bacterial load in mice. It effectively treats lethal infections caused by clinically isolated strains of Pseudomonas aeruginosa (Acinetobacter baumannii), Klebsiella pneumoniae, and Escherichia coli (E. coli).

LB 11058 is a novel injectable cephalosporin featuring a C-3 pyridyl-substituted vinyl sulfide and a C-7 2-amino-5-chloro-1,3-thiazole group. This compound exhibits exceptional activity against Streptococcus pneumoniae and demonstrates similar efficacy against β-hemolytic streptococci. The inhibition pattern for LB 11058 with S. aureus is consistent, as all isolates are inhibited under this pattern.

YFJ-36 is an antibiotic that demonstrates superior and broad-spectrum antibacterial activity in vitro compared to cefiderocol, particularly against A. baumannii and K. pneumoniae. In a systemic infection model in mice, YFJ-36 exhibits strong in vivo efficacy. Additionally, the compound shows enhanced physicochemical stability in liquid media with a pH of 6-8 and is noteworthy for its potential to reduce allergy risk due to its quaternary ammonium bond.

DNA Gyrase-IN-15 (Compound 11) is an antibacterial agent that inhibits both DHPS and DNA gyrase, with IC50 values of 1.73 and 0.07 µM, respectively. It shows antimicrobial activity against Enterococcus faecium (MIC of 15.62 µg/mL), Acinetobacter baumannii, Enterobacter (MIC of 7.81 µg/mL), Pseudomonas aeruginosa, Klebsiella pneumoniae, and Staphylococcus aureus. Additionally, DNA Gyrase-IN-15 exhibits antibiofilm activity against Enterococcus faecium.

KPC-IN-1 (compound 1e) is an inhibitor of Klebsiella pneumoniae carbapenemase KPC-2, with an IC50 value of 8.3 nM. KPC is a β-lactamase expressed in Gram-negative bacteria that hydrolyzes carbapenems, leading to significant bacterial resistance to carbapenem antibiotics.