Antibacteriano

<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>Diploicin is a dibenzofuran lactone compound with activity against Gram-positive bacteria, found in lichens (lichens).</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>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>Cefclidin (Cefclidine) is a cephalosporin compound.</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>LpxA-IN-1, a novel UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitor exhibiting potent activity (IC 50 2 nM), effectively targets Pseudomonas aeruginosa</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>Antibacterial agent 80 (compound 20) has antibacterial activity [1].</p>

<p>SPR719 is an inhibitor of gyrase B, has bactericidal 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>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>LpxH-IN-2 (compound 014), a potent inhibitor of LpxH, exhibits antibacterial activity against E. coli.</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>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>1,5-Dideoxy-1,5-imino-D-mannitol is an antibiotic with antibacterial properties.</p>

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

<p>Antibacterial agent 113 targets multiple bacteria including P. aeruginosa and E. coli, showing efficacy at MIC 15625 μM.</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>MtTMPK-IN-1 inhibits MtTMPK with 2.5 μM IC50, shows moderate anti-tuberculosis activity, and is low in cytotoxicity.</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>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>Antitubercular agent-22 combats Candida albicans (MIC: 2.34 μg/ml) and M. tuberculosis (MIC: 2 μg/ml).</p>

<p>HT1171 is a potent and selective inhibitor of the Mycobacterium tuberculosis proteasome. It exhibits strong antitubercular activity against Mycobacterium tuberculosis H37Rv, with a MIC90 of 2 μg/mL and MIC of 4 μg/mL. At a concentration of 100 μM, HT1171 shows an inhibition rate of 53.8% against normal human liver cells (L02). HT1171 is applicable in antituberculosis drug research.</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>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>FtsZ-IN-4 is an oral FtsZ inhibitor with strong antibacterial effects and good drug traits, low toxicity (CC50 &gt;20μg/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>(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>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>JPL is an InhA-cofactor-ligand 3FNG inhibitor and is used for the study of tuberculosis [1].</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>Antitubercular agent-15 (5n): low toxicity, fights M. tuberculosis strains; MIC90 values range 0.73-18.8 μg/mL.</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>Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.</p>

<p>PKZ18 is an antibiotic that inhibits bacterial growth with a MIC value of 32-64 μg/mL against most Gram-positive bacteria. It suppresses the in vivo transcription and translation of glycyl-tRNA synthetase mRNA. PKZ18 selectively targets stem I specifier loops in Gram-positive bacteria, directly reducing T-box transcription readthrough of associated genes. It prevents codon-anticodon pairing necessary for tRNA binding and is less likely to induce resistance.</p>

<p>GT-055 (LCB18-055) is a novel inhibitor of broad-spectrum β-lactamase.</p>

<p>DNA Gyrase-IN-1: potent, selective promoter inhibitor. IC50: 2.6 μM, inhibits Mtb, MIC: 0.49 μM. Useful for tuberculosis research.</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>Elongation factor P-IN-2, a β-lysine derivative, is a potent EFP inhibitor reducing E. coli growth.</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>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>ACHN-975 TFA is a selective LpxC inhibitor with a subnanomolar inhibitory. It is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL).</p>

<p>RCB18350 is an antituberculosis agent and an isoxazole derivative. It demonstrates bacteriostatic properties by inhibiting the growth of Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 1.25 μg/mL. RCB18350 is effective against multi-drug resistant Mycobacterium tuberculosis (MDR-TB) clinical isolates, Mycobacterium bovis BCG, and Mycobacterium avium, all of which are slow-growing mycobacteria.</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>QPX7728 methoxy acetoxy methy ester is an inhibitor of boronic acid β-lactamase.</p>

<p>vacuolar H+-ATPases (V-ATPases) inhibitor</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>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>8-Hydroxyerythromycin A is a semi-synthetic antibiotic with antibacterial activity.</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>Finafloxacin is a pH-activated fluoroquinolone, most effective at pH 5.0-6.0, targeting bacterial topoisomerases, used for UTIs and H. pylori 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>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>Antibacterial agent 82 (compound 7p) is an antibacterial agent [1].</p>

<p>G247 inhibits MsbA by keeping NBDs apart, blocking ATPase activity.</p>

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

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

<p>TB inhibitor 4, a spirothiazolidinone from mandelic acid, blocks 98% of M. tuberculosis H37Rv under 6 μg/mL.</p>

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

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

<p>BRD-4592 is an allosteric inhibitor targeting tryptophan synthase (TrpAB) of Mycobacterium tuberculosis. It binds at the α-β subunit interface of TrpAB, with an IC50 of 70.9 nM for the α subunit and 22.6 nM for the β subunit.</p>

<p>(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.</p>

<p>MtTMPK-IN-9 moderately inhibits MtbTMPK (IC50: 48 μM), has submicromolar Mycobacterium activity, and is non-toxic, aiding tuberculosis research.</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>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>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>Antibacterial agent 68 targets drug-resistant E. coli at 0.007 mM with low cytotoxicity.</p>

<p>Antibacterialagent 278 (compound B1) is an antimicrobial agent that exhibits potent inhibitory activity against Gram-positive bacteria.</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>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>NusB-IN-1 (22r) is an oral bacterial rRNA inhibitor, effective against MRSA and VRSA.</p>

<p>Antibacterial agent 90 (6n), a pleuromutilin derivative, targets Gram-positive pathogens and Mycoplasma pneumoniae.</p>

<p>14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase with antibacterial activity.</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>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>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>PqsR-IN-2, potent PqsR inhibitor, curbs Pseudomonas aeruginosa communication, reduces pyocyanin, with low toxicity.</p>

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

<p>PF 03709270 is an oral prodrug of sulopenem with broad-spectrum antibacterial effects on gram-positive and gram-negative bacteria.</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>Streptothricin F is a biochemical.</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>Ph-Ph+ is a dimerized phenanthroline derivative with antitumor, antibacterial, and antifungal effects.</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>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>Compound 8b inhibits VEGFR-2/DHFR, combats various bacteria, and fights cancer cells.</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>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>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>GSK656 (GSK3036656) inhibits Mtb LeuRS with IC50 of 0.20 μM, promising for tuberculosis treatment.</p>