Antibactérien

JPL is an InhA-cofactor-ligand 3FNG inhibitor and is used for the study of tuberculosis [1].

Altersolanol A (Stemphylin; NSC 173943) demonstrates effective antimicrobial properties, inhibiting the growth of Bacillus subtilis and Pseudomonas aeruginosa with a minimum inhibitory concentration (MIC) ranging from 25-100 μg/mL. Additionally, it shows no phytotoxic effects on Taxus at a concentration of 4 μg/μL.

(E)-Cefodizime ((E)-THR-221) is an antibiotic that selectively binds to penicillin-binding proteins (PBPs), inhibiting bacterial cell wall synthesis, which results in its antibacterial activity. It holds potential for research into various bacterial infections, including the prevention of preoperative infections.

<p>BioA-IN-1 (Compound 15) is an inhibitor of the key enzyme BioA in the biotin biosynthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. It exhibits antibacterial activity without cytotoxicity.</p>

<p>Compound 174 (Compound 5g), an antibacterial agent, exhibits potent anti-infective properties in vivo along with appreciable pharmacokinetic profiles. This highly active substance demonstrates favorable biofilm removal capabilities, low hemolysis, and acceptable mammalian cell toxicity [1].</p>

<p>LpxA-IN-1, a novel UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitor exhibiting potent activity (IC 50 2 nM), effectively targets Pseudomonas aeruginosa</p>

Antimicrobial Agent-29 (Compound C35) influences the interaction between human hemoglobin and the Staphylococcus aureus IsdB hemophore. This compound facilitates the identification of IsdB:Hb PPI inhibitors [1].

HC2210 exhibits antibacterial effects against Mycobacterium abscessus (Mab) with an EC50 of 0.72 µM. It modulates the expression of Mab genes associated with oxidative stress and lipid metabolism. HC2210 is applicable for studies on Mab infections.

Metallo-β-lactamase-IN-14 (Compound 17e) serves as an inhibitor of Metallo-β-Lactamase, displaying inhibitory activity against VIM-1 and VIM-2. This compound also exhibits antibacterial effects on Gram-negative (GN) bacteria and P. aeruginosa [1].

Antibacterial Agent 172 (Compound 6a), a <i>Clostridioides difficile (Cd) SpoVD inhibitor with an IC50 value of 89 nM, effectively inhibits the sporulation of Clostridioides difficile. It is useful for research on bacterial infections [1].

NBTI 5463 is a bacterial type II topoisomerase (topoisomerase II) inhibitor with antimicrobial properties. It effectively inhibits GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. By binding to topoisomerase II, NBTI 5463 prevents DNA cleavage and re-ligation, thereby impeding bacterial DNA replication and transcription. This compound shows potential for research into Gram-negative bacterial infections.

844-TFM, a NBTI DNA gyrase blocker, IC50: 1.5 μM, kills Mycobacterium abscessus.

Aztreonam-siderophore conjugate 63 is an antibacterial agent that exhibits efficacy against Gram-negative bacteria through the linkage of aztreonam to a

OPC-167832: oral dprE1 inhibitor, IC50 0.258 μM, anti-tuberculosis, for Mycobacterium tuberculosis research.

DNA gyrase B-IN-1, a potent inhibitor of P. aeruginosa DNA gyrase B, has IC50 of 2.2 μM with high affinity and stability.

FR-145715 is a histamine H2 receptor antagonist characterized by its specific anti-Helicobacter pylori activity. This compound is utilized in the study of gastric lesions.

TAN-1057C is a potent antibiotic with antimicrobial activity against both Gram-negative and Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA).

(1S,2R,7S)-Sitafloxacin (DU-6856) is an enantiomer of Sitafloxacin and functions as a topoisomerase inhibitor. As an antibiotic, it demonstrates inhibitory activity against Escherichia coli DNA gyrase (IC50 0.18 μg/mL) and Staphylococcus aureus topoisomerase IV. (1S,2R,7S)-Sitafloxacin exhibits antibacterial properties and is utilized in the study of various bacterial infections.

Apalcillin (PC-904) combined with Ro 48-1220 (a penicillin sulfone β-lactamase inhibitor) exhibits broad-spectrum activity against Gram-negative aerobic and anaerobic bacteria, excluding Klebsiella acid-producing strains. This combination shows strong efficacy against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae with an effective MIC of 11 μg/mL. Additionally, it inhibits Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter at low MICs (0.25 to 4 μg/mL). However, it has limited efficacy against oxacillin-resistant staphylococci and some Gram-positive bacteria. Apalcillin/Ro 48-1220's effectiveness against certain extended-spectrum β-lactamase-producing Escherichia coli is comparable to piperacillin/tazobactam, though it is less effective against SHV-type β-lactamases.

Aquayamycin is an anthraquinone derivative and inhibitor of the enzyme tyrosine hydroxylase..