Antibactérien

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

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

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

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

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.

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>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>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>

(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.

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

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

AVE-1330A sodium is a beta-Lactamase inhibitor.

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

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>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>

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.

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>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>

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

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

<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>

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].

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.

Fostriecin inhibits PP2A/PP4 (IC50s = 3.2/3 nM), weakly affects topoisomerase II/PP1 (IC50s = 40/131 μM), doesn't inhibit PP2B, and may modify epigenetics.

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

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

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.

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

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

2-Bromo-2'-methoxyacetophenone acts as an irreversible inhibitor of MurA, effectively inhibiting MurA in E. coli with an IC50 of 0.38 μM. This compound helps inhibit bacterial cell wall synthesis, making it useful in antimicrobial research.

<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>

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.

QPX7728 bis-acetoxy methyl ester is an inhibitor of boronic acid β-lactamase.

<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>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>

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.

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

<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>

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

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.

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>

2-Mercaptopyridine N-oxide sodium is a useful organic compound for research related to life sciences. The catalog number is T66776 and the CAS number is 3811-73-2.

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

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

Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.

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

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

Dusquetide is a first-in-class innate defense regulator. Dusquetide displays activity in both reducing inflammation and increasing the clearance of bacterial infection.

Xibornol (Nanbacine) 具有广谱的抗菌和抗病毒活性，可用于研究革兰氏阳性菌感染和人呼吸道合胞病毒与人冠状病毒229E感染。

Phosalacine, isolated from Kitasatosporia phosalacinea, is a new herbicidal antibiotic that contains phosphinothricin.

<p>Pulcherriminic acid, a cyclic dipeptide, chelates Fe3+, forms pulcherrimin, and has antimicrobial properties used in food, agriculture, and medicine.</p>

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

N-(3-(Dimethylamino)propyl)tetradecanamide is a useful organic compound for research related to life sciences. The catalog number is T66531 and the CAS number is 45267-19-4.

Bacampicillin hydrochloride is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin.

Ramifenazone is a drug of nonsteroidal anti-inflammatory.

CRS3123 (REP-3123) dihydrochloride is an orally active, fully synthetic antimicrobial agent that effectively inhibits Clostridioides difficile methionyl-tRNA synthetase (MetRS). CRS3123 dihydrochloride can be used in the study of Clostridioides difficile infection (CDI).

N-Butylthiophosphoric triamide is a useful organic compound for research related to life sciences. The catalog number is T65336 and the CAS number is 94317-64-3.

1-Cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid is a useful organic compound for research related to life sciences. The catalog number is T66948 and the CAS number is 112811-72-0.

1-Naphthalenemethanol is a natural product for research related to life sciences. The catalog number is T67143 and the CAS number is 4780-79-4.

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

MuRF1-IN-2 (Example 3) is a MuRF1 inhibitor used to study conditions linked to muscle wasting, encompassing both skeletal and cardiac muscle atrophy [1].

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].

Ulifloxacin is a useful organic compound for research related to life sciences. The catalog number is T65577 and the CAS number is 112984-60-8.

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.

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.

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).

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.

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

Ciprofloxacin lactate is a useful organic compound for research related to life sciences. The catalog number is T66299 and the CAS number is 97867-33-9.

<p>TP0586532 is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.</p>

d-Atabrine hydrochloride is the active enantiomer of quinacrine and has anti-pr virus activity.

Ribocil-C is a selective inhibitor of the bacterial riboflavin riboswitch, a synthetic analogue of flavin mononucleotide (FMN), inhibits bacterial cell growth.