Antibactérien

<p>Cetefloxacin (E 4868) is a broad-spectrum antibacterial antibiotic with a minimum inhibitory concentration (MIC) ranging from 0.007 to 8 µg/ml. In mice, cetefloxacin demonstrates favorable pharmacokinetic properties and provides protection against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.</p>

<p>MtTMPK-IN-1 inhibits MtTMPK with 2.5 μM IC50, shows moderate anti-tuberculosis activity, and is low in cytotoxicity.</p>

<p>Antitubercular agent-23 combats Candida albicans (MIC: 1.1 μg/ml) and M. tuberculosis (MIC: 1 μg/ml).</p>

<p>Antibacterial agent 79 is an antibacterial agent.</p>

<p>Ibafloxacine (R835) is a fluoroquinolone antibiotic that is used exclusively in veterinary applications and shows zero good bacteriostatic effect against</p>

<p>Enzyme-IN-3 disodium (compound 7) is a selective inhibitor of Mycobacterium tuberculosis shikimate kinase with an IC50 of 1.6 μM. Additionally, Enzyme-IN-3 disodium exhibits antibacterial properties.</p>

<p>epi-D-Captopril (epi-D-SQ 14225) is a stereoisomer of Captopril and functions as an inhibitor of metallo-beta-lactamases (MBLs). The IC50 values of epi-D-Captopril for NDM-1, IMP-1, and VIM-2 are 64 μM, 173 μM, and 5.5 μM, respectively. This compound holds potential for research in MBLs-related antibiotic-resistant infections.</p>

<p>WQ3810 is an orally active fluoroquinolone, has potent antibacterial activities.</p>

<p>RNAP-σ interaction inhibitor-1 (compound 5d) acts as an inhibitor of the interaction between RNA polymerase and the sigma factor. It exhibits activity against Streptococci with a minimum inhibitory concentration (MIC) ranging from 1-2 µg/mL.</p>

<p>2'-Amino-2'-deoxyadenosine (9-(2-Amino-2-deoxypentofuranosyl)-9H-purin-6-amine) is a nucleoside antibiotic that effectively inhibits various Mycoplasma strains.</p>

<p>Meclocycline: a tetracycline antibiotic, inhibits LDH, reduces cell toxicity from mutant huntingtin, doesn't change protein levels in PC12 cells.</p>

<p>Antibacterial agent 75 re-sensitizes VRSA to vancomycin.</p>

<p>Urease -IN-1 is a urease inhibitor (IC50: 2.21±0.45 μM).</p>

<p>Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent with low cytoxicity for MCF-7, A549 cells [1].</p>

<p>Nitrovin is an antimicrobial growth promoter that induces ROS-mediated non-apoptotic and quasi-apoptotic cell death by targeting TrxR1. It exhibits anticancer activity with IC50 values ranging from 1.31 to 6.60 μM for both tumor and normal cells.</p>

<p>Streptothricin F is a biochemical.</p>

<p>TBAJ-5307 is a broad-spectrum anti-non-tuberculous mycobacteria inhibitor that targets the FO-domain of the engine, preventing rotation and proton-translocation. TBAJ-5307 inhibits non-tuberculous mycobacteria in vitro and in vivo [1].</p>

<p>BDM91288, an orally active AcrB efflux pump inhibitor of pyridinium piperazine, enhances the in vivo efficacy of levofloxacin in treating Klebsiella pneumoniae pulmonary infection in mouse models [1].</p>

<p>5,6-Dihydro-5-azathymidine exhibits activity against both Gram-positive and Gram-negative bacteria, as well as DNA viruses.</p>

<p>Anti-MRSA agent 23 (compound 11) is a potent agent against methicillin-resistant Staphylococcus aureus. This compound exhibits both antibacterial and antibiofilm properties. It facilitates the healing and reconstruction of MRSA-infected skin wounds by reducing bacterial load, alleviating inflammation, and promoting angiogenesis.</p>

<p>Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma.</p>

<p>NDM-1 Inhibitor-5 (compound 57) exhibits strong inhibition of NDM-1, characterized by a K i of 2.5 μM. Additionally, it demonstrates synergistic antibacterial effects when combined with meropenem [1].</p>

<p>Levofloxacin mesylate is an orally active antibiotic effective against both Gram-positive and Gram-negative bacteria. It inhibits DNA gyrase and topoisomerase IV enzymes. Levofloxacin mesylate is employed in research related to chronic periodontitis, airway inflammation, and BK viremia. Additionally, it possesses anti-Orthopoxvirus activity.</p>

<p>Antibacterial agent 204 (Compd P2-56-3) enhances the activity of Rifampin (RIF) against Acinetobacter baumannii and Klebsiella pneumoniae by disrupting the outer membrane of A. baumannii. T [1].</p>

<p>DL-2-Aminopimelic Acid acts as a weak agonist for glutamate receptors and also reduces the sensitivity of leech glutamate receptors to glutamate.</p>

<p>Compound 3d: antitubercular, MIC 0.007 μg/mL vs MTB H37Rv, 1.851 μg/mL vs MDR-MTB 16833, metabolically unstable.</p>

<p>Antibacterial agent 81 blocks DNA transcription, targets S. aureus (MIC 12.5μM) &amp; M. smegmatis (MIC 7.8μM). Used in infection research.</p>

<p>Pneumolysin-IN-1 (compound PB-3), characterized as a targeted small molecule inhibitor of Pneumolysin (PLY) with an IC50 value of 3.1 µM, acts as a pore-blocking agent and an anti-virulence factor. This compound is useful for researching infections caused by Streptococcus pneumoniae [1].</p>

<p>LasR antagonist 1 (Compound 7), with an IC50 of 0.4 μM, is an effective antagonist of LasR that modulates quorum sensing (QS) in the opportunistic pathogen Pseudomonas aeruginosa [1].</p>

<p>L 689065 is a 5-lipoxygenase inhibitor.</p>

<p>MA220607 is an antibacterial agent characterized by low hemolytic toxicity and a dual-target mechanism of action (MOA). It promotes FtsZ protein polymerization, increases bacterial membrane permeability, and inhibits biofilm formation. The resistance rate of MA220607 is low, with MICs against Gram-positive bacteria and Gram-negative bacteria ranging from 0.062-2 μg/mL and 0.5-4 μg/mL, respectively [1].</p>

<p>Xeruborbactam isoboxil is a β-lactamase (beta-lactamase) inhibitor.</p>

<p>Diploicin is a dibenzofuran lactone compound with activity against Gram-positive bacteria, found in lichens (lichens).</p>

<p>HKI12134085 (compound 3), an orally administered nitrobenzothiazinone (BTZ) derivative, demonstrates antibacterial efficacy against Mycobacterium tuberculosis. This compound exhibits significant in vivo inhibitory potency within a BALB/c mouse model of Mycobacterium tuberculosis infection [1].</p>

<p>Mt KARI-IN-1 inhibits Mtb KARI with a 3.06 μM Ki, targeting tuberculosis.</p>

<p>Antitubercular agent-15 (5n): low toxicity, fights M. tuberculosis strains; MIC90 values range 0.73-18.8 μg/mL.</p>

<p>N-Cbz-L-Cysteine (Cbz-cysteine) (compound 5) functions as a potent inhibitor of β-lactamase II, exhibiting a K i value of 97 µM [1].</p>

<p>QPX7728 bis-acetoxy methyl ester is an inhibitor of boronic acid β-lactamase.</p>

<p>Ro 24-4383 is a carbamate-linked dual-action antibacterial agent.</p>

<p>BRL-42715 is an effective inhibitor of bacterial beta-lactamases.</p>

<p>MBL-IN-5 is an inhibitor of metallo-β-lactamase (MBL). It effectively suppresses three clinically significant B1 subfamily MBLs: NDM-1, VIM-1, and IMP-1 with IC50 values of 0.05 nM, 14 nM, and 21 nM respectively. MBL-IN-5 notably enhances the efficacy of carbapenem antibiotics against MBL-producing clinical strains and, when combined with IPM antibiotics, significantly reduces bacterial load in a thigh infection model.</p>

<p>MK-3402 is a metallo-beta-lactamase inhibitor. MK-3402can be used in the research of bacteria .</p>

<p>Antifungal agent 38, a heterocyclic disulfide, shrinks hyphae and damages cell membranes, causing leakage.</p>

<p>H052 is a selective inhibitor of Staphylococcus aureus α-hemolysin (Hla). It binds to the Hla monomer, disrupting its interaction with the host cell membrane, thereby blocking pore formation and inhibiting calcium influx, cytotoxicity, and inflammatory response. H052 exhibits inhibitory activity against Hla-induced calcium influx (EC50 = 30 nM in U937 cells) and holds potential for research into lung infections caused by S. aureus.</p>

<p>LasR-IN-1 (9g) strongly inhibits LasR, potent vs E. coli, with a 28.13 μM MIC against P. aeruginosa.</p>

<p>OSUAB-0284 is an inhibitor of bacterial topoisomerase. It exhibits significant activity against staphylococci, particularly methicillin-resistant Staphylococcus aureus (MRSA). The compound exerts its antibacterial effect by inhibiting bacterial topoisomerase and may be used in research on infections caused by drug-resistant bacteria, including MRSA.</p>

<p>Antibacterialagent 278 (compound B1) is an antimicrobial agent that exhibits potent inhibitory activity against Gram-positive bacteria.</p>

<p>Palmitanilide (Palmitic acid anilide) is an antimicrobial agent effective against Gram-positive bacteria. It can electrostatically bind to components of the cell wall of Gram-positive bacteria (such as Bacillus cereus), altering the membrane structure and affecting normal cellular functions. Palmitanilide shows potential for research into infections caused by Gram-positive bacteria.</p>

<p>(R)-ZG197: Activates Sa ClpP (EC50=1.5μM) &amp; Hs ClpP (EC50=31.4μM); selective for Sa ClpP.</p>

<p>Cefclidin (Cefclidine) is a cephalosporin compound.</p>

<p>Eravacycline (TP-434) is a potent and broad-spectrum antibacterial agent.</p>

<p>Piperacillin hydrate is a semisynthetic broad-spectrum β-lactam antibiotic. It exhibits potent bactericidal activity against Gram-negative bacteria and some Gram-positive bacteria by targeting penicillin-binding proteins. Piperacillin hydrate is frequently combined with the β-lactamase inhibitor Tazobactam for enhanced efficacy.</p>

<p>MsbA-IN-2 is a potent inhibitor of the lipopolysaccharide transporter MsbA and is able to act on E. coli MsbA (IC50: 2 nM).</p>

<p>BAR-072 is a small molecule inhibitor targeting TraE with a KD value of 2.7 µM. It significantly suppresses the transfer of the antibiotic resistance-associated plasmid pKM101. BAR-072 holds promise as a candidate molecule for research in disease areas related to infection and resistance control, by inhibiting the spread of bacterial resistance genes.</p>

<p>(S)-ZG197 is a compound that acts as a highly selective activator of the Staphylococcus aureus Caseinolytic Protease P (Sa ClpP), demonstrating efficacy at a</p>

<p>Aurachin C is a quinoline alkaloid belonging to the isoprenoid class, known for its antimalarial, antifungal, and antibacterial properties. It acts as a selective terminal oxidase inhibitor.</p>

<p>Antibacterial agent 169 (Compound 28), a pyrrolamide-type GyrB/ParE inhibitor, exhibits antibacterial properties by inhibiting Gyrase and Topo IV in Staphylococcus aureus. It has IC 50 values of 49 nmol/L and 1.513 μmol/L, respectively [1].</p>

<p>Metallo-β-lactamase-IN-13 (Compound 13i) serves as a pan Metallo-β-Lactamase inhibitor with extended activity against Gram-negative (GN) bacteria expressing metallo-β-lactamases. It exhibits antibacterial properties effective against P. aeruginosa [1].</p>

<p>Asukamycin, from S. nodosus asukaensis, is a polyketide antibiotic inhibiting tumor cells by activating caspases 8 and 3.</p>

<p>Compound 7b (Antibacterial agent 99) is an effective agent with antibacterial, antifungal properties and no haemolytic activity.</p>

<p>InhA-IN-7 (Compound 11), a derivative of Triclocan, shows inhibitory activity against enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. It effectively inhibits the proliferation of both wildtype and mutant strains of Mycobacterium tuberculosis, exhibiting minimum inhibitory concentrations (MICs) ranging from 19 to 75 μM [1].</p>

<p>Antibacterial agent 113 targets multiple bacteria including P. aeruginosa and E. coli, showing efficacy at MIC 15625 μM.</p>

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

<p>RNAP-σ interaction inhibitor-2 (compound 7d) is an inhibitor targeting the interaction between RNA polymerase and the sigma factor. It demonstrates inhibitory activity against S. aureus with a minimum inhibitory concentration (MIC) of 2 µg/mL.</p>

<p>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.</p>

<p>Anti-MRSA agent 3 targets MRSA with 0.098 μg/ml MIC, low toxicity, binds DNA, and disrupts cell walls/membranes.</p>

<p>SPR719 is an inhibitor of gyrase B, has bactericidal activity.</p>

<p>1,5-Dideoxy-1,5-imino-D-mannitol is an antibiotic with antibacterial properties.</p>

<p>Antibacterial agent 80 (compound 20) has antibacterial activity [1].</p>

<p>LpxH-IN-2 (compound 014), a potent inhibitor of LpxH, exhibits antibacterial activity against E. coli.</p>

<p>Doxazosin impurity 12 acts as an inhibitor of CTX-M β-lactamase (Beta-lactamase) with a Ki value of 0.7 mM against CTX-M.</p>

<p>CM-728 is an oxazanonaphthoquinone that exhibits cytotoxic and antibacterial properties. It acts as a human peroxidase-1 inhibitor and serves as a source of oxidative stress affecting mitochondrial function.</p>

<p>NDM-1 inhibitor-3 is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor (Ki : 4 μM) widely found in nature and is associated with antibiotic resistance.</p>

<p>14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase with antibacterial activity.</p>

<p>DNA Gyrase-IN-16 (Compound 9) is an inhibitor of DNA gyrase, with an IC50 of 1.609 μM. It exhibits antibacterial properties, effectively inhibiting S. aureus and MRSA, with a MIC of 3.125 μM for both.</p>

<p>Anti-MRSA agent 2 inhibits MRSA at 0.098 μg/ml, with low toxicity and disrupts bacterial membranes and DNA.</p>

<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>Penethamate hydriodide is a diethylaminoethyl ester prodrug of penicillin, utilized via intramuscular injection to treat mastitis in cattle.</p>

<p>Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.</p>

<p>L-threo-β-Hydroxyaspartic acid is an amino acid antibiotic with activity against Bacillus subtilis, Xanthomonas oryzae, Mycobacterium phlei, and Botrytis cinerea.</p>

<p>EFP-IN-1: potent β-lysine derivative, inhibits EFP, slows E. coli growth.</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>QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.</p>

<p>Carumonam Sodium is a monobactam, penicillin-binding protein inhibitor. It is used as antibacterials.</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>

<p>MCB-3681, active against gram-positive bacterium, is the antibacterial Oxaquin's active substance.</p>

<p>LY 215890 is a compound that exhibits potent Gram-negative and Gram-positive antibacterial activity.</p>

<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].</p>

<p>BAS-118 is a benzamide derivative exhibiting antibacterial activity. For 100 randomly selected strains of Helicobacter pylori, its MIC50, MIC90, and MIC range were ≤0.003, 0.013, and ≤0.003-0.025 mg/L, respectively. BAS-118 shows potential for research as an anti-H. pylori agent.</p>

<p>β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric inhibitor targeting β-glucuronidase. It exhibits potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) with an IC50 of 12.9 nM. The compound exerts its inhibitory effect through reversible covalent modification of cysteine residues (Cys28, Cys443, and Cys197) on EcGUS. It is applicable in research on gut microbiota-related diseases, particularly in reducing the toxic side effects of Irinotecan and non-steroidal anti-inflammatory drugs (NSAIDs).</p>

<p>Colistin adjuvant-1, inhibits NF-κB (IC50: 0.209 μM), boosts mucin against gram-negative bacteria.</p>

<p>Compound 11: Sulfonylurea derivative, antimicrobial, anticancer; MIC 0.039-0.156 mg/mL; A549 IC50: 19.7 μg/mL, PC3 IC50: 11.9 μg/mL.</p>

<p>KKL-40 is a small-molecule inhibitor that targets the trans-translation process, effectively suppressing methicillin-sensitive and resistant Staphylococcus aureus (S. aureus) and other Gram-positive pathogens, including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. It works in synergy with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not show synergistic effects with other antibiotics such as daptomycin, kanamycin, or erythromycin. KKL-40 inhibits trans-translation, an extreme form of recoding, while being non-toxic to HeLa cells.</p>

<p>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].</p>

<p>DC-159a, an 8-methoxy fluoroquinolone, possesses broad-spectrum antibacterial activity, with a particular efficacy against Gram-positive pathogens. The MIC90 values for DC-159a are 0.5 μg/mL against Streptococcus anginosus group, 4 μg/mL against Clostridium difficile, and 2 μg/mL against Bacteroides fragilis.</p>

<p>NDM-1 inhibitor-7 (Compound A8) is an NDM-1 inhibitor with an IC50 of 10.284 μM. It restores the ability of meropenem (MEM) to penetrate the cell wall of Gram-negative bacteria and effectively reinstates MEM's antibacterial activity against NDM-1 positive Escherichia coli. Moreover, NDM-1 inhibitor-7 demonstrates significant efficacy in both Galleria mellonella and murine peritonitis infection models.</p>

<p>Antibacterial Agent 172 (Compound 6a), a &lt;i&gt;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].</p>

<p>AAA-10 formic is an orally active inhibitor of intestinal bacterial bile salt hydrolase (BSH) against B.</p>

<p>Anticaries agent-1 (Compound 21b) is utilized as an anticaries agent. It effectively inhibits biofilm formation with an IC50 of 77 μM and restricts the growth of S. mutans.</p>

<p>Bilanafos is an agent of Anti-Bacterial.</p>