Antibacteriano

<p>Glutamate-5-kinase-IN-2 (compound 54) is a potent G5K inhibitor with 4.2 μM MIC, potential in anti-TB research.</p>

<p>Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding to the PqsR protein. It suppresses the expression of quorum sensing system-related genes lasB, rhlA, and pqsA, thereby preventing the production of virulence factors elastase, pyocyanin, and rhamnolipid. Quorum sensing-IN-9 disrupts the motility of P. aeruginosa, inhibits biofilm formation, and reduces the bacterium's virulence and pathogenicity. Additionally, it exhibits anti-infective activity in the Galleria mellonella larval model.</p>

<p>MsbA-IN-4 (Compound 32) is a highly selective and potent inhibitor of MsbA (IC50: 3 nM).MsbA-IN-4 inhibits Escherichia coli (MIC: 12 μM).</p>

<p>Dioxidine is an antimicrobial agent that can inhibit bacterial growth. It is utilized in research on pyogenic infections.</p>

<p>Anti bacterial agent 236 (Compound 4l), an orally effective inhibitor of DNA gyrase and topoisomerase IV (with IC50 values of 3.2 and 300 nM in Staphylococcus aureus, respectively), exhibits broad-spectrum antibacterial activity. It also demonstrates favorable pharmacokinetic properties in mice.</p>

<p>KPC-2-IN-2 (6c) inhibits KPC-2 enzyme in Klebsiella pneumoniae (Ki 0.038 μM) and boosts cefotaxime in E. coli KPC-2.</p>

<p>Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg/mL, and exhibits anti-tuberculosis activity.</p>

<p>Aurantiogliocladin is a mild antibiotic effective against Staphylococcus epidermidis, but it shows no efficacy against Staphylococcus aureus. It is also capable of inhibiting biofilm formation.</p>

<p>LolCDE-IN-2 is a potent Lol protein (LolCDE) inhibitor. LolCDE-IN-2 shows antibacterial activity with a MIC of 2 μg/ml against E. coli MG1655 [1].</p>

<p>PptT-IN-1, a potent PptT inhibitor (IC50: 2.8 μM), shows promise for tuberculosis research.</p>

<p>9-tert-Butyldoxycycline exhibits immunomodulatory activity by altering the polarization state of polymorphonuclear neutrophils and ameliorating inflammatory responses in ischemia-reperfusion injury models. Additionally, 9-tert-Butyldoxycycline serves as a ligand for the "Tet-On" inducible gene expression system.</p>

<p>7-APRA is a semisynthetic intermediate of the cephalosporin class of antibiotics. It exhibits antibacterial activity and is primarily used in the synthesis of other cephalosporin antibiotics, such as Cefaclor and Cefprozil.</p>

<p>Compound 4e, an antibacterial against P. aeruginosa, disrupts cell membranes (MIC: 1 μg/ml).</p>

<p>Anti-MRSA agent 27 (compound 4a) is a potent antimicrobial agent against methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 0.0975 μmol/L. It effectively disrupts MRSA biofilms and inhibits the production of hemolysins.</p>

<p>LasR-IN-2 blocks LasR via H-bond with TRY-56, useful in bacterial infection and CF research.</p>

<p>β-Glucuronidase-IN-2 is a potent inhibitor of E.</p>

<p>Mycobacterium Tuberculosis-IN-6 (compound b1) is an inhibitor of the enoyl reductase InhA from Mycobacterium tuberculosis, with an IC50 value of 7.74 μM. It is useful in antibacterial research.</p>

<p>Antibacterial agent 87 is an effective antibacterial agent that acts on MRSA (MIC: 0.125 μg/ml), MRSE (MIC: 0.0625 μg/ml) and S. aureus (MIC: 0.0625 μg/ml).</p>

<p>Pisiferic acid is a novel PP2C activator and an an antimicrobial diterpenoid</p>

<p>FtsZ-IN-4 is an oral FtsZ inhibitor with strong antibacterial effects and good drug traits, low toxicity (CC50 &gt;20μg/mL).</p>

<p>G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter protein. G092 has potential for antibacterial drug research.</p>

<p>Antitubercular agent-22 combats Candida albicans (MIC: 2.34 μg/ml) and M. tuberculosis (MIC: 2 μg/ml).</p>

<p>Lapyrium chloride (Emcol E 607) is a broad-spectrum antibacterial agent that serves as a preservative and disinfectant.</p>

<p>Compound 6q, a trifluoromethylpyridine oxadiazole, targets Xanthomonas oryzae with EC50 of 7.2 μg/mL.</p>

<p>Mazethramycin is an antitumor antibiotic that exerts its effects by disrupting DNA replication and RNA synthesis within cells. It is utilized in cancer research.</p>

<p>MsbA-IN-3 is a potent and highly selective MsbA inhibitor (IC50: 2 nM). MsbA-IN-3 inhibits Escherichia coli activity (MIC: 35 μM).</p>

<p>MraY-IN-2 (compound 6) is an effective inhibitor of bacterial transposase MraY (IC50=4.5 μ M), and can be used for antibacterial research.</p>

<p>BM635 hydrochloride, an MmpL3 inhibitor, strongly blocks Divergent bacteriophage H37Rv (MIC50: 0.08 μM), with doubled in vivo potency.</p>

<p>Gln-AMS (TFA) is a type Ia amido-tRNA synthetase (AARS) inhibitor with a Ki value of 1.32 μM for glutaminyl-tRNA synthetase.</p>

<p>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.</p>

<p>MtTMPK-IN-9 moderately inhibits MtbTMPK (IC50: 48 μM), has submicromolar Mycobacterium activity, and is non-toxic, aiding tuberculosis research.</p>

<p>Antibiofilm agent-4 is a LasR inhibitor, demonstrating optimal antibiofilm and anti-QS (quorum sensing) properties.</p>

<p>HldA/E-IN-1 (compound 8) is a dual inhibitor of HldA/E, exhibiting IC50 values of 17.2 μM and 67.8 μM, respectively. This compound is utilized in research on antibacterial infections.</p>

<p>FPI-1465: Dual serine-β-lactamase &amp; PBP inhibitor; IC50 PBP2=1.0 μg/mL; Kd CTX-M-15=0.011μM, OXA-48=5.3μM.</p>

<p>MBX-1162, a bis-indole compound, has demonstrated unique substrate specificity related to MepA and MepR in studies investigating its resistance mechanisms in Staphylococcus aureus. It has not shown cross-resistance with related compounds.</p>

<p>Ph-Ph+ is a dimerized phenanthroline derivative with antitumor, antibacterial, and antifungal effects.</p>

<p>ZG297 is an agonist of Staphylococcus aureus ClpP (SaClpP) with an EC50 of 0.26 μM. It degrades SaFtsZ and inhibits bacterial cell division, exhibiting antistaphylococcal activity by inhibiting S. aureus 8325-4 and MRSA strains, with a MIC range of 0.063-256 μg/mL. In mouse models, ZG297 demonstrates anti-infective properties.</p>

<p>MsbA-IN-1: Potent MsbA inhibitor (IC50: 4 nM), anti-E. coli (MIC: 79 μM), penetrates Gram-negative bacteria.</p>

<p>Compound 112: Powerful antibacterial, MIC 1250 μM against B. subtilis, E. coli, E. faecalis, S. typhimurium, S. aureus; also an HIV-1 antibody.</p>

<p>K13787 is an acetohydroxy acid synthase (AHAS) inhibitor with antibacterial properties. It exhibits antimicrobial activity against various non-tuberculous mycobacteria (NTM) as well as clarithromycin (CLR) resistant strains.</p>

<p>DNA Gyrase-IN-13 (compound 1b) is an inhibitor of DNA gyrase with bacteriostatic properties. It exhibits an IC50 of 1.81 μM against Staphylococcus aureus DNA gyrase.</p>

<p>Squalamine lactate is an aminosterol compound discovered in the tissues of the dogfish shark, with antimicrobial activity.</p>

<p>Kikumycin A, an antibiotic produced by Streptomyces, exhibits antimicrobial activity against both Gram-positive and Gram-negative bacteria. Additionally, it demonstrates antitrichomonal activity with a minimum inhibitory concentration (MIC) of 25 μg/mL against Trichomonas foetus.</p>

<p>Glutamate-5-kinase-IN-1 is a potent G5K inhibitor with a 4.1 μM MIC, showing promise in anti-TB research.</p>

<p>MT0703 is a cephalosporin antibiotic featuring an aminothiazolylglycyl moiety with a 1,5-dihydroxy-4-pyridinone-2-carbonyl group, displaying potent activity against Pseudomonas species.</p>

<p>Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.</p>

<p>Antibacterialagent 259 (K3) is a bactericide with EC50 values of 1.5, 1.7, and 4.9 mg/L against Xoo, Xoc, and Xac, respectively. It induces the production of reactive oxygen species (ROS) in pathogens, leading to their death. Antibacterialagent 259 is applicable in research for controlling bacterial diseases in plants.</p>

<p>Cefempidone (GR 50692) is a third-generation cephalosporin antibiotic. It exhibits antibacterial activity by inhibiting penicillin-binding proteins involved in the synthesis of bacterial cell walls.</p>

<p>Pks13-TE inhibitor 4 (compound 44) is a potent inhibitor from the thiazole series that effectively targets Pks13 to combat tuberculosis (TB) and addresses drug resistance.</p>

<p>Fenbenicillin (Phenbenicillin) potassium is a semi-synthetic penicillin with antibacterial spectrum activity.</p>