Antibacterial

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

<p>Antibacterial agent 79 is an antibacterial agent.</p>

<p>WQ3810 is an orally active fluoroquinolone, has potent antibacterial activities.</p>

<p>QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.</p>

<p>RNAP-σ interaction inhibitor-1 (compound 5d) acts as an inhibitor of the interaction between RNA polymerase and the sigma factor. It exhibits activity against Streptococci with a minimum inhibitory concentration (MIC) ranging from 1-2 µg/mL.</p>

<p>Antibacterial agent 75 re-sensitizes VRSA to vancomycin.</p>

<p>Urease -IN-1 is a urease inhibitor (IC50: 2.21±0.45 μM).</p>

<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>5,6-Dihydro-5-azathymidine exhibits activity against both Gram-positive and Gram-negative bacteria, as well as DNA viruses.</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>

<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>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>

<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>

<p>L 689065 is a 5-lipoxygenase inhibitor.</p>

<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>

<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>

<p>Xeruborbactam isoboxil is a β-lactamase (beta-lactamase) inhibitor.</p>

<p>Mt KARI-IN-1 inhibits Mtb KARI with a 3.06 μM Ki, targeting tuberculosis.</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>

<p>HKI12134085 (compound 3), an orally administered nitrobenzothiazinone (BTZ) derivative, demonstrates antibacterial efficacy against Mycobacterium tuberculosis. This compound exhibits significant in vivo inhibitory potency within a BALB/c mouse model of Mycobacterium tuberculosis infection [1].</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>(S)-ZG197 is a compound that acts as a highly selective activator of the Staphylococcus aureus Caseinolytic Protease P (Sa ClpP), demonstrating efficacy at a</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>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>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>Antibacterialagent 278 (compound B1) is an antimicrobial agent that exhibits potent inhibitory activity against Gram-positive bacteria.</p>

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

<p>(R)-ZG197: Activates Sa ClpP (EC50=1.5μM) &amp; Hs ClpP (EC50=31.4μM); selective for Sa ClpP.</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>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>Compound 7b (Antibacterial agent 99) is an effective agent with antibacterial, antifungal properties and no haemolytic activity.</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>

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

<p>SPR719 is an inhibitor of gyrase B, has bactericidal activity.</p>

<p>Antibacterial agent 80 (compound 20) has antibacterial activity [1].</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>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>NDM-1 inhibitor-3 is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor (Ki : 4 μM) widely found in nature and is associated with antibiotic resistance.</p>

<p>Anti-MRSA agent 2 inhibits MRSA at 0.098 μg/ml, with low toxicity and disrupts bacterial membranes and DNA.</p>

<p>Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.</p>

<p>BioA-IN-1 (Compound 15) is an inhibitor of the key enzyme BioA in the biotin biosynthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. It exhibits antibacterial activity without cytotoxicity.</p>

<p>EFP-IN-1: potent β-lysine derivative, inhibits EFP, slows E. coli growth.</p>

<p>Carumonam Sodium is a monobactam, penicillin-binding protein inhibitor. It is used as antibacterials.</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>MCB-3681, active against gram-positive bacterium, is the antibacterial Oxaquin's active substance.</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>LY 215890 is a compound that exhibits potent Gram-negative and Gram-positive antibacterial activity.</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>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>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>Dioxidine is an antimicrobial agent that can inhibit bacterial growth. It is utilized in research on pyogenic infections.</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>PptT-IN-1, a potent PptT inhibitor (IC50: 2.8 μM), shows promise for tuberculosis research.</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>G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter protein. G092 has potential for antibacterial drug research.</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>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>Ph-Ph+ is a dimerized phenanthroline derivative with antitumor, antibacterial, and antifungal effects.</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>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>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>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>(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>Fabimycin, a FabI inhibitor, combats drug-resistant gram-negative bacterial infections effectively.</p>

<p>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.</p>

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

<p>MtTMPK-IN-1 inhibits MtTMPK with 2.5 μM IC50, shows moderate anti-tuberculosis activity, and is low in cytotoxicity.</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>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>MtTMPK-IN-9 moderately inhibits MtbTMPK (IC50: 48 μM), has submicromolar Mycobacterium activity, and is non-toxic, aiding tuberculosis research.</p>

<p>Antitubercular agent-15 (5n): low toxicity, fights M. tuberculosis strains; MIC90 values range 0.73-18.8 μg/mL.</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>DC-159a, an 8-methoxy fluoroquinolone, possesses broad-spectrum antibacterial activity, with a particular efficacy against Gram-positive pathogens. The MIC90 values for DC-159a are 0.5 μg/mL against Streptococcus anginosus group, 4 μg/mL against Clostridium difficile, and 2 μg/mL against Bacteroides fragilis.</p>

<p>Anticaries agent-1 (Compound 21b) is utilized as an anticaries agent. It effectively inhibits biofilm formation with an IC50 of 77 μM and restricts the growth of S. mutans.</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>Diploicin is a dibenzofuran lactone compound with activity against Gram-positive bacteria, found in lichens (lichens).</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>GT-055 (LCB18-055) is a novel inhibitor of broad-spectrum β-lactamase.</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>Streptothricin F is a biochemical.</p>

<p>Meclocycline: a tetracycline antibiotic, inhibits LDH, reduces cell toxicity from mutant huntingtin, doesn't change protein levels in PC12 cells.</p>

<p>Ibafloxacine (R835) is a fluoroquinolone antibiotic that is used exclusively in veterinary applications and shows zero good bacteriostatic effect against</p>

<p>Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent with low cytoxicity for MCF-7, A549 cells [1].</p>

<p>Antitubercular agent-23 combats Candida albicans (MIC: 1.1 μg/ml) and M. tuberculosis (MIC: 1 μg/ml).</p>

<p>Anthelvencin A is a pyrrolylamide metabolite with moderate antibacterial and anthelmintic activity.</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>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>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>MsbA-IN-5 (compound 40) is a potent and highly selective inhibitor of MsbA (IC50: 2 nM). MsbA-IN-5 can be used in Gram-negative studies.</p>

<p>Antibiofilm agent-14 (compound 11) functions as an antibiofilm agent. It exhibits antifungal activity against C.albicans SC5314, with a minimum inhibitory concentration (MIC) of 50 μM.</p>

<p>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.</p>

<p>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).</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 76 (compound 9) is a potent antibacterial agent.</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>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>

<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>MtTMPK-IN-8 inhibits MtbTMPK, has low cytotoxicity, shows 0.78-9.4 μM activity against Mycobacterium, useful for tuberculosis research.</p>

<p>ACHN-975: potent LpxC inhibitor with subnanomolar activity; targets many gram-negative bacteria; MIC ≤1 μg/mL.</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>Antibacterial agent 68 targets drug-resistant E. coli at 0.007 mM with low cytotoxicity.</p>

<p>(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium TFA (Compound 4a) functions as a Gram-negative outer membrane permeabilizer by targeting Met47 in LptA to disrupt LptA/LptC interactions, exhibiting synergistic antibacterial activity. This compound, when in the form of (trifluoromethanesulfonate), enhances the efficacy of pol B against both wild-type and multi-drug resistant A. baumannii and E. coli strains. Additionally, (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) serves as an adjuvant for antibiotics combating multi-drug resistant Gram-negative bacteria.</p>