Antibactérien

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

<p>Compound 6xa inhibits drug-resistant tuberculosis with MICs 0.03 μg/mL for DS-Mtb and 0.03-0.06 for DR-Mtb, SI&gt;40 for Vero cells.</p>

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

<p>7-Hydroxytropolone (3-Hydroxytropolone) is an antibiotic that exhibits activity against Gram-positive and Gram-negative bacteria, as well as yeasts and fungi. It also functions as an inhibitor of 2''-O-adenylate transferase.</p>

<p>(4-Aminobenzoyl)-D-glutamic acid (Compound 17) exhibits competitive inhibitory activity against the H2-pterin synthesis system, affecting folic acid synthesis and subsequently inhibiting bacterial growth.</p>

<p>Avibactam sodium dihydrate (NXL-104) is a reversible covalent inhibitor for CTX-M-15 and TEM-1 β-lactamases with IC50s of 5 nM and 8 nM.</p>

<p>Antibacterial agent 78 (compound 30) is an antibacterial agent with improved cytotoxicity profile[1].</p>

<p>Antifungal agent 27 shows moderate action against MRSA, weak against C. albicans, with MICs of 8 μg/mL and 32 μg/mL, respectively.</p>

<p>PF 03709270 is an oral prodrug of sulopenem with broad-spectrum antibacterial effects on gram-positive and gram-negative bacteria.</p>

<p>Antibacterial agent 88 is an effective antibacterial agent against B. subtilis (MIC: 4 μg/ml) with MIC values of ≤0.0156 μg/mL for MRSA, MRSE and S. aureus.</p>

<p>Compound 5q is a potent antitubercular with low MIC90 values (0.40-23.51 μg/mL) against M. tuberculosis strains, showing minimal cytotoxicity.</p>

<p>Compound 8b inhibits VEGFR-2/DHFR, combats various bacteria, and fights cancer cells.</p>

<p>Elongation factor P-IN-2, a β-lysine derivative, is a potent EFP inhibitor reducing E. coli growth.</p>

<p>N6-Benzoyl-2'-deoxyadenosine monohydrate is a nucleoside analogue that helps diagnose bacterial infections by binding to double-stranded DNA and altering its structure, which can subsequently be detected using electrophoresis.</p>

<p>VEGFR-2/DHFR-IN-2 inhibits VEGFR-2 &amp; DHFR (IC50: 0.623 &amp; 9.085 μM), toxic to C26, HepG2, MCF7 cells (IC50: 3.59-8.38 μM), promising for cancer study.</p>

<p>Rubropunctatin is a monascus pigment with very potent cancer cell proliferation inhibitory effects.</p>

<p>BM635 mesylate inhibits MmpL3; kills Divergent bacterium with 0.6 µM MIC50; boosts bioavailability.</p>

<p>(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>

<p>RmlA-IN-2: Strong RmlA blocker, hinders l-rhamnose synthesis &amp; alters bacterial wall permeability (IC50: 0.303 μM).</p>

<p>Antibacterial agent 118, potent against various mycobacteria, has MIC values ranging from 10.2 to 163.0 μM. Useful in TB research.</p>

<p>LpxC-IN-10 is a selective LpxC inhibitor with an MIC of 0.5 μg/mL against E. coli and K. pneumoniae and is capable of being used to study bacterial infections.</p>

<p>LasR-IN-3 inhibits LasR in Pseudomonas, disrupting its dimer, causing loss of function.</p>

<p>PqsR-IN-2, potent PqsR inhibitor, curbs Pseudomonas aeruginosa communication, reduces pyocyanin, with low toxicity.</p>

<p>MtMetAP1-IN-1 is an inhibitor of methionine aminopeptidase 1 ( MetAP1 ). MtMetAP1-IN-1 shows antimycobacterial activity.</p>

<p>MtTMPK-IN-3 inhibits Mycobacterium tuberculosis kinase with IC50 0.12μM, MIC 12.5μM on Mtb, cytotoxic EC50 12.5μM on MRC-5 cells.</p>

<p>FG-2101 is a selective, orally active non-hydroxamate LpxC inhibitor with an IC50 of approximately 1 nM. It demonstrates exceptional selectivity over other bacterial and human metalloproteases. FG-2101 is useful for studying infections caused by Gram-negative bacteria, including resistant strains.</p>

<p>Antibacterial agent 77 (compound 12) is an antibacterial agent [1].</p>

<p>GSK656 (GSK3036656) inhibits Mtb LeuRS with IC50 of 0.20 μM, promising for tuberculosis treatment.</p>

<p>PptT-IN-3 (5p), an inhibitor of PptT in Mycobacterium tuberculosis, IC50=3.5μM, is key for TB research.</p>

<p>Cefoxazole is a β-lactam antibiotic featuring an isoxazole structure, known for its antibacterial activity. It can be utilized in the study of infectious diseases.</p>

<p>RhlR antagonist 1: IC50 of 26 μM, selective for RhlR, inhibits P. aeruginosa biofilm and virulence factors.</p>

<p>MRL-494, a small-molecule BamA inhibitor, resists efflux and outer membrane permeability, with antibacterial properties.</p>

<p>MtTMPK-IN-7 inhibits MtbTMPK (IC50: 47 μM), active against M. brevis (MIC: 2.3-4.7 μM), useful for tuberculosis research.</p>

<p>Antitubercular agent-11 (Compound 1e) is an antitubercular agent with a bulkier electron-donating group (Bu-t) that shows the best MIC value of 0.060 μg/mL [1].</p>

<p>Antibacterialagent 279 (compound A12) is an effective antibacterial agent. It inhibits the SOS response of Pseudomonas aeruginosa.</p>

<p>MtTMPK-IN-2 inhibits M. tuberculosis TMPK (IC50: 1.1 μM), Mtb H37Rv (MIC: 12.5 μM), and is cytotoxic in MRC-5 cells (EC50: 6.1 μM).</p>

<p>Compound 11i: potent, non-toxic anti-tuberculosis biphenyl analogue.</p>

<p>NFC nitro probe 1 (compound 18) is a chemical probe designed for the detection of Mtb, exhibiting high potency against both R-Mtb and NR-Mtb.</p>

<p>Probenecid sodium is the sodium salt of Probenecid, a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Additionally, Probenecid acts as an inhibitor of pannexin 1 channels.</p>

<p>Atramycin A is an anthraquinone antibiotic with antitumor properties.</p>

<p>Novel anti-TB agent 62 is a redox compound with bactericidal activity against active and dormant bacteria.</p>

<p>Antibacterialagent 262 (compound A23) is a potent antibacterial agent that inhibits the activity of Xanthomonas oryzae pv oryzae. It also disrupts the integrity of bacterial cell membranes by preventing the formation of biofilms of Xanthomonas oryzae pv oryzae.</p>

<p>Cephalosporin C exhibits relatively weak resistance to Gram-positive and Gram-negative bacteria. It is stable against penicillinase, but can be decomposed by cephalosporinase. When hydrolyzed to remove its side chain, it yields 7-amino-cefenoic acid (7-ACA), which is an essential raw material for the production of semisynthetic cephalosporins.</p>

<p>Colistin adjuvant-2 is a compound that acts as a potentiation agent for colistin, effectively enhancing its activity against Gram-negative bacteria [1].</p>

<p>MurA-IN-6 (Compound L16) is a selective MurA inhibitor with an IC50 of 26.63 μM. It exhibits antibacterial activity by inhibiting the function of MurA, a key protein essential for bacterial cell wall synthesis.</p>

<p>4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.</p>

<p>NBTIs-IN-5 inhibits Mycobacterium abscessus DNA with IC50 1.5μM, halts growth at MIC90 0.4μM.</p>

<p>Deprodone is an active compound that inhibits key processes such as bacterial cell wall synthesis by interacting with hydrolase and transferase proteins of methicillin-resistant Staphylococcus aureus (MRSA). It is applied in the research of MRSA infections, inflammatory skin diseases, intestinal disorders, and fatty acid metabolism disorders.</p>

<p>Diclosulam (XDE 564) is an herbicide with a Ki value of less than 32 nM. It exhibits a MIC of 6.25 and 12.5 μM, and a MIC50 of 1.40 and 3.01 μM against the CBS10913 and CBS12373 strains, respectively.</p>

<p>Anthelvencin A is a pyrrolylamide metabolite with moderate antibacterial and anthelmintic activity.</p>

<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>

<p>Compound 20P is a potent antibacterial, inhibits biofilms with IC50 4.5 μM, and reduces pyocyanin at IC50 8.6 μM.</p>

<p>ROS inducer 9 (compound 4e) is an antibacterial agent with a minimum inhibitory concentration (MIC) of 0.25 μg/mL against Escherichia coli. It eradicates bacteria by inhibiting GSH activity and increasing ROS levels. Additionally, ROS inducer 9 exhibits low toxicity toward red blood cells and RAW 264.7 cells.</p>

<p>(R)-Sitafloxacin (DU-6857) is an enantiomer of Sitafloxacin (DU-6859a) and functions as a topoisomerase inhibitor, demonstrating an IC50 of 0.18 μg/mL against DNA gyrase.</p>

<p>Benzisothiazolone is an isothiazolinone fungicide that demonstrates growth inhibitory activity against Escherichia coli ATCC 8739 and yeast NCYC 1354. It is utilized in studies investigating growth inhibition models.</p>

<p>Keto lovastatin is an impurity of lovastatin with antibacterial properties. Lovastatin is a cell-permeable HMG-CoA reductase (HMG-CoA reductase) inhibitor used to reduce cholesterol levels.</p>

<p>AK-968-11563024 is an inhibitor targeting marine V. vulnificus NAT [(VIBVN)NAT] with an IC50 value of 18.86 µM. In V. vulnificus, NAT (aromatic amine N-acetyltransferase) plays a role in drug metabolism, contributing to drug resistance. Thus, AK-968-11563024 can be used for research related to drug tolerance.</p>

<p>Thiolactomycin is a novel reversible dual inhibitor of D-amino acid oxidase (DAO) and D-Aspartate oxidase (DDO).</p>

<p>Lavendomycin can be extracted from Streptomyces lavendulae and has active against Gram-positive bacteria.</p>

<p>MtTMPK-IN-5 inhibits Mtb TMPK with IC50 of 34 μM and fights tuberculosis with MIC of 12.5 μM, aiding TB research.</p>