Antibactérien

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

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].

Penethamate hydriodide is a diethylaminoethyl ester prodrug of penicillin, utilized via intramuscular injection to treat mastitis in cattle.

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

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

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.

L-threo-β-Hydroxyaspartic acid is an amino acid antibiotic with activity against Bacillus subtilis, Xanthomonas oryzae, Mycobacterium phlei, and Botrytis cinerea.

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.

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

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.

QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.

(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.

Cefclidin (Cefclidine) is a cephalosporin compound.

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

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

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].

NusB-IN-1 (22r) is an oral bacterial rRNA inhibitor, effective against MRSA and VRSA.

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

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].

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

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.

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

Antimicrobial agent-38 (compound 10) effectively inhibits methicillin-resistant Staphylococcus aureus (S. aureus) strain ATCC 700699 and non-resistant strain ATCC 29213, with minimum inhibitory concentrations (MIC) of 32 mg/L and 64 mg/L, respectively.

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

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.

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.

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

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.

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

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.

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

2'-Amino-2'-deoxyadenosine (9-(2-Amino-2-deoxypentofuranosyl)-9H-purin-6-amine) is a nucleoside antibiotic that effectively inhibits various Mycoplasma strains.

Levofloxacin mesylate is an orally active antibiotic effective against both Gram-positive and Gram-negative bacteria. It inhibits DNA gyrase and topoisomerase IV enzymes. Levofloxacin mesylate is employed in research related to chronic periodontitis, airway inflammation, and BK viremia. Additionally, it possesses anti-Orthopoxvirus activity.

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

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

Antitubercular agent-15 (5n): low toxicity, fights M. tuberculosis strains; MIC90 values range 0.73-18.8 μg/mL.

MK-3402 is a metallo-beta-lactamase inhibitor. MK-3402can be used in the research of bacteria .

Trans-Clopenthixol ((E)-Clopenthixol) is an antibiotic without any sedative properties. It can be used in vitro to inhibit Pseudomonas aeruginosa and Plasmodium falciparum.

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

Antibacterialagent 266 (Compound C5) is an inhibitor of plant pathogenic bacteria that disrupts the integrity of bacterial cell membranes. It exhibits an EC50 of 24.1 μg/mL against Xanthomonasoryzaepvoryzae (Xoo) and 39.0 μg/mL against X. axonopodispvcitri (Xac). Antibacterialagent 266 is valuable for research in plant pathology and the development of agricultural antibacterial agents.

MB076 is an innovative heterocyclic triazole designed with enhanced plasma stability. It effectively inhibits seven distinct Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with K i values less than 1 μM. Additionally, MB076 demonstrates a synergistic effect when combined with various cephalosporins to restore pBCSK(−) susceptibility [1].

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.

BAR-072 is a small molecule inhibitor targeting TraE with a KD value of 2.7 µM. It significantly suppresses the transfer of the antibiotic resistance-associated plasmid pKM101. BAR-072 holds promise as a candidate molecule for research in disease areas related to infection and resistance control, by inhibiting the spread of bacterial resistance genes.

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

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.

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

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

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

Ro 24-4383 is a carbamate-linked dual-action antibacterial agent.

BRL-42715 is an effective inhibitor of bacterial beta-lactamases.

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.

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.

Antibacterialagent 281 (Compound 95,186) effectively inhibits the growth of GAS by binding to the ligand-binding pocket of SPs0871, competing with the ligand. It exhibits concentration-dependent growth inhibition against Streptococcus pyogenes (S. pyogenes).

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

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.

Aquayamycin is an anthraquinone derivative and inhibitor of the enzyme tyrosine hydroxylase..

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].

epi-D-Captopril (epi-D-SQ 14225) is a stereoisomer of Captopril and functions as an inhibitor of metallo-beta-lactamases (MBLs). The IC50 values of epi-D-Captopril for NDM-1, IMP-1, and VIM-2 are 64 μM, 173 μM, and 5.5 μM, respectively. This compound holds potential for research in MBLs-related antibiotic-resistant infections.

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.

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.

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

NBTI 5463 is a bacterial type II topoisomerase (topoisomerase II) inhibitor with antimicrobial properties. It effectively inhibits GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. By binding to topoisomerase II, NBTI 5463 prevents DNA cleavage and re-ligation, thereby impeding bacterial DNA replication and transcription. This compound shows potential for research into Gram-negative bacterial infections.

Antibacterial agent 77 (compound 12) is an antibacterial agent [1].

Antibacterial agent 68 targets drug-resistant E. coli at 0.007 mM with low cytotoxicity.

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.

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.

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.

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.

Urease-IN-16, with an IC50 of 132 µmol/L, is a urease inhibitor that coordinates with nickel atoms through the oxygen atoms of either carbonyl or boronic acid groups. This compound holds significant potential as an additive in the development of efficient fertilizers and medical applications.

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.

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

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).

Carbonic anhydrase inhibitor28 (Compound 11) serves as an inhibitor for the Pseudomonas aeruginosa carbonic anhydrase. It exhibits antibacterial activity, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 0.5 and 1 μg/mL, respectively, against P. aeruginosa. Carbonic anhydrase inhibitor28 is utilized in research focused on anti-infection applications.

β-Glucuronidase-IN-2 is a potent inhibitor of E.

Urease-IN-2 is a non-competitive inhibitor of urease (IC50: 0.94 μM, Ki: 1.6 μM) that non-competitively inhibits Jack bean urease (JBU).

(-)-15-Deoxyspergualin is a potent antitumor agent that demonstrates significant inhibition against mouse leukemia L-1210.

Anthelvencin A is a pyrrolylamide metabolite with moderate antibacterial and anthelmintic activity.

Pisiferic acid is a novel PP2C activator and an an antimicrobial diterpenoid

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.

(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.

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

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

MtDTBS-IN-1 is a notably potent binder (K_D = 57 nM) and inhibitor (K_i = 5 μM) of MtDTBS.

(R)-ZG197: Activates Sa ClpP (EC50=1.5μM) & Hs ClpP (EC50=31.4μM); selective for Sa ClpP.

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

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.

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.

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

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).

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

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.

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

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.

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

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.

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).

Streptothricin F is a biochemical.

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].

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