Antibacteriano

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

Antibacterialagent 261 (compound 43) is a potent inhibitor of the peptide deformylase (PDF) enzyme, demonstrating IC50 values of 2.5 nM against Staphylococcus aureus (S. aureus) and 10.6 nM against Escherichia coli (E. coli).

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

<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>

DNA Gyrase-IN-1: potent, selective promoter inhibitor. IC50: 2.6 μM, inhibits Mtb, MIC: 0.49 μM. Useful for tuberculosis research.

<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>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>

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

MraY-IN-3 (12a) is a potent inhibitor of the bacterial translocase MraY (IC50: 140 μM). 46 μg/ml).

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

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

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

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

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.

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

<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>

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.

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.

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

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>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>1,5-Dideoxy-1,5-imino-D-mannitol is an antibiotic with antibacterial properties.</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>QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.</p>

Cilastatin ammonium salt is an antibiotic that is particularly effective against Gram-positive cocci, with a half-life of 3-4 hours.

MetRS-IN-1 (Compound 27) is an inhibitor of E. coli methionyl-tRNA synthetase (MetRS) with an IC50 value of 237 nM [1].

<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>SPR719 is an inhibitor of gyrase B, has bactericidal activity.</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>Antibacterial agent 80 (compound 20) has antibacterial activity [1].</p>

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

<p>FtsZ-IN-13 (Compound C11) functions as an inhibitor of the temperature-sensitive mutant Z (FtsZ), exhibiting IC50 values of 47.97 μM for FtsZSa and 34 μM for FtsZPa. It demonstrates notable antibacterial activity against Staphylococcus aureus (with a minimum inhibitory concentration of 2 μg/mL), cystic fibrosis Staphylococcus aureus clinical isolates, and methicillin-resistant Staphylococcus aureus (MRSA). FtsZ-IN-13 is applicable in research on antibiotic resistance.</p>

Rf470 (Rotor NO.4) TFA is an FMR-probe-D-lysine conjugate (Max Ex: 470 nM; Max Em: 640 nM) that can be covalently integrated into bacterial peptidoglycan. In its free state, Rf470 TFA exhibits weak fluorescence, which significantly increases upon integration into peptidoglycan by transpeptidase catalysis. This fluorescence change allows Rf470 TFA to be used for real-time monitoring of peptidoglycan biosynthesis, detecting transpeptidase activity, and screening antibiotics.

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.

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

<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>

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>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>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>

Fabimycin, a FabI inhibitor, combats drug-resistant gram-negative bacterial infections effectively.

<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>

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

QPX7728 methoxy acetoxy methy ester is an inhibitor of boronic acid β-lactamase.

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

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

Eravacycline (TP-434) is a potent and broad-spectrum antibacterial agent.

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

vacuolar H+-ATPases (V-ATPases) inhibitor

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

8-Hydroxyerythromycin A is a semi-synthetic antibiotic with antibacterial activity.

<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>

PptT-IN-2 inhibits PptT enzyme crucial in tuberculosis, with 2.5 μM IC50, showing potential in TB research.

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

<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>

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>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>

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>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>

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

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

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

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).

Citric acid-13C2 is a 13C-labeled form of citric acid. Citric acid serves as a preservative and food additive. It induces apoptosis in HaCaT cells and causes cell cycle arrest at the G2/M and S phases. Additionally, citric acid contributes to liver oxidative damage by reducing antioxidant enzyme activity. It also functions as an acidulant, emulsifier, chelating agent, and buffer, with extensive applications across multiple industries.

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

<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>

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.

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>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>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>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>

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

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

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

PqsR-IN-1, potent PqsR inhibitor, curbs pyocyanin in Pseudomonas aeruginosa with low cytotoxicity.

<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>

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].

<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>

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>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>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>Tigemonam is a monobactam, a novel orally administered monobactam that protects against gram-negative aerobic bacterial pathogens. Cost-effective and quality-assured.</p>

<p>LeuRS-IN-1 hydrochloride is a Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with antileukemic activity and antimalarial activity.</p>

Gepotidacin mesylate dihydrate (GSK2140944 mesylate dihydrate) is an antibiotic and an inhibitor of bacterial type II topoisomerase.

<p>Eravacycline dihydrochloride (TP-434-046) is a potent and broad-spectrum antibacterial agent against six E. coli (MICs: 0.125-0.25 mg/L).</p>

<p>Durlobactam sodium salt (ETX2514) have an IC50 values of 4, 14 and 190 nM against class A KPC-2, class C AmpC and class D OXA-24.Cost-effective and quality-assured.</p>

Reutericyclin is a unique tetramic acid, is an antibiotic produced by some strains of Lactobacillus reuteri.

Bicyclomycin benzoate (BCM benzoate, FR2054) is a broad-spectrum antibiotic and selective Rho protein inhibitor active against Gram-negative bacteria.

<p>Terpineol possesses antifungal activity against Trichophyton mentagrophytes, it also exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria. α-Terpineol (Terpineol) shows anticonvulsant, and anti-inflammatory activities, it inhibits the gene expression of the IL-6 receptor.</p>

<p>Cefetamet pivoxyl, a cephalosporin antibiotic, effectively inhibits 355 enteropathogens, including Gram-negative bacteria (ausgenommen Pseudomonas aeruginosa) and Legionella pneumophila [1].</p>

Ramifenazone is a drug of nonsteroidal anti-inflammatory.

Pseudomonic acid C is the analogue of Pseudomonic Acid D which is an antibiotic agent from Pseudomonas fluorescens.

<p>Sulfamonomethoxine sodium is a long-acting sulfonamide antibacterial agent utilized in blood kinetic studies; it inhibits dihydropteroate synthetase, thereby blocking folic acid synthesis [1].</p>

Hexahydrohippuric acid is a useful organic compound for research related to life sciences. The catalog number is T65235 and the CAS number is 32377-88-1.

Ethyl 4-hydroxy-2-methyl-2H-benzo[e][1,2]thiazine-3-carboxylate 1,1-dioxide is a useful organic compound for research related to life sciences. The catalog number is T65688 and the CAS number is 24683-26-9.

PqsR/LasR-IN-1 (Compound 2a) is a potent inhibitor of LasR and PqsR systems in P. aeruginosa. PqsR/LasR-IN-1 is also a inhibitor of hERG (IC50= 6.77 μM).

l-Atabrine dihydrochloride displays antiprion activity. l-Atabrine dihydrochloride is a less active enantiomer of quinacrine.

<p>Trans-Clopenthixol dihydrochloride ((E)-Clopenthixol dihydrochloride), an antibiotic without neuroleptic effects, has demonstrated in vitro efficacy against Pseudomonas aeruginosa and Plasmodium falciparum, as referenced in [1] [2].</p>

Oleandomycin, a macrolide antibiotic structurally similar to Erythromycin, exhibits antimicrobial activity.

<p>Cefadroxil is a first generation aminocephalosporin with good patient compliance, a long-acting therapeutic effect, high solubility and relatively broad spectrum of anti-bacterial activity. Cefadroxil is also a substrate of the intestinal peptide transporter PepT1, which is primarily responsible for the drug's uptake across the apical membrane of small intestine.</p>

<p>Compound GK02084(SC) may have activity against the GTP site of Bs‐FtsZ.</p>

<p>Lenampicillin hydrochloride is an orally active prodrug of Ampicillin. Lenampicillin hydrochloride is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins. It is applied in the investigation of suppurative skin </p>