Antibacteriano

<p>BO 2367, a topoisomerase inhibitor, is used to suppress the growth of tumor .</p>

<p>DHFR-IN-10 (compound 4c) is a potent inhibitor of dihydrofolate reductase (DHFR), displaying an inhibition concentration half-maximum (IC50) of 4.21 μM against</p>

<p>Elastase LasB-IN-1 (Compound 4b), a potent and selective inhibitor of elastase LasB, exhibits antibacterial activity and has been determined to possess an IC50</p>

<p>AG 85 is a major secretion protein of Mycobacterium tuberculosis.</p>

<p>Antibiofilm Agent-2 (Compound 4T) serves as a potent biofilm inhibitor, exhibiting an IC50 of 3.6 μM, and impairs the quorum sensing system along with iron</p>

<p>β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.</p>

<p>MAC13772 is a potent inhibitor of the enzyme BioA with an IC50 of 250 nM thereby inhibiting biotin biosynthesis. MAC13772 exhibits antibacterial activity.</p>

<p>LtaS-IN-1 inhibits LTA synthesis in MDR E. faecium; alters cell walls; MIC: 0.5-64 μg/mL for 28 Enterococcus strains.</p>

<p>Streptovitacin A boosts growth inhibition against fungi.</p>

<p>Isotianil is a plant defense inducer that activates typical plant defense responses without direct antimicrobial effects, serving as a plant protection agent</p>

<p>Methyl 2-amino-5-bromobenzoate (Methyl 5-Bromoanthranilate) is an HCV NS5b RNA polymerase inhibitor with antimicrobial activity.</p>

<p>Δ2-transEicosenoic acid, an α,β-unsaturated fatty acid, emerges as a by-product during the synthesis of Δ2-ciseicosenoic acid, which along with its salts, shows promise in diabetes treatment and lipid metabolism enhancement. Additionally, the compound 2-octadecenoic acid is recognized for its ability to enhance liver function and reduce blood sugar levels in streptozocin-induced diabetic rats.</p>

<p>Mtb-IN-4 (compound 17h) is a non-toxic isoxazole that exhibits anti-Mycobacterium tuberculosis (Mtb) activity, with an IC50 value of 0.70 μM.</p>

<p>17(R)-Resolvin D4 (17(R)-RvD4) is an epimer of RvD4, generated through the aspirin-induced modification process.</p>

<p>Variculanol, a compound with antimicrobial, anticancer, and anti-HCV NS3/4A protease properties, is derived from the marine fungus Aspergillus versicolor [1].</p>

<p>Rosoxacin (Acrosoxacin) shows antibacterial activities against a broad spectrum of Gram-negative bacteria including Neisseria gonorrhoeae (MIC90 = 0.03mg/ml).</p>

<p>Antituberculosis agent-8: MIC 3.53 μM vs M. tuberculosis, antifungal MIC 62.50 μM vs A. niger.</p>

<p>Tuberculosis inhibitor 6 (compound 2c), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, is highly active against Mycobacterium tuberculosis (MIC 90 of</p>

<p>T145 halts key bacteria growth at sub μg/ml, deters resistance, and may enhance drug lifespan.</p>

<p>Lithium benzoate, an aromatic alcohol present in numerous plants, commonly serves as an additive in food, beverages, cosmetics, and various other products. This compound exhibits antibacterial and antifungal properties, functioning effectively as a preservative [1].</p>

<p>DQn-1, a potent antifolate, demonstrates efficacy against Mycobacterium tuberculosis (Mtb) with an MIC 90 of 0.03 µM.</p>

<p>Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on</p>

<p>L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.</p>

<p>LS-BF1: Stable, low-toxic antimicrobial peptide targeting ESKAPE pathogens via cell membrane disruption, effective in mouse infection model.</p>

<p>G43-C3-TEG is a glycosyl-transferase inhibitor that diminishes biofilm formation by inhibiting the synthesis of extracellular polysaccharides (EPS) [1].</p>

<p>Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and</p>

<p>Compound 158 (6c), a Micrococcin analogue, serves as an antibacterial agent effective against impetigo and Clostridium difficile infection (CDI) [1].</p>

<p>LY 173013 is a bicyclic pyrazolidinone, it has antibacterial properties.</p>

<p>1,8-Dichloroanthraquinone, a derivative of anthraquinone, effectively inhibits sulfide production in sulfate-reducing bacteria [1].</p>

<p>SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM.</p>

<p>Compound 5b, an antibacterial, effectively targets MRSA and disrupts bacterial membranes and PG synthesis.</p>

<p>TP0480066 inhibits topoisomerase II, DNA gyrase (IC50=1.1nM), topo IV (IC50=62.89nM), effective against drug-resistant bacteria and N. gonorrhoeae.</p>

<p>NSC309401 is an E. coli dihydrofolate reductase inhibitor, displaying potency with an IC50 value of 189 nM and a dissociation constant (KD) of 14.57 nM [1].</p>

<p>BLI-489 hydrate is a penicillin β-lactamase inhibitor that acts on classes A and C and some class D β-lactamases.</p>

<p>Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci,</p>

<p>Micronomicin (Gentamicin C2b) is an antibiotic exhibiting antibacterial and bactericidal capacity.</p>

<p>L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.</p>

<p>Butylparaben sodium significantly impacts the later phases of spermatogenesis in the testes by impairing hormonal regulation and/or RNA and protein synthesis [1</p>

<p>ThrRS-IN-3: Potent inhibitor of Salmonella enterica ThrRS, IC50 = 19 nM, Kd = 34 nM, with antibacterial effects.</p>

<p>Biotin-cholesterol, a biotinylated derivative of cholesterol, serves as a precursor in the manufacturing of biotin-conjugated liposomes and micelles, which are utilized in drug delivery systems [1].</p>

<p>BAY-Y 3118, a new chlorofluoroquinolone, has antimicrobial activity.</p>

<p>Anti-MRSA Agent 8 (Compound 7g), a derivative of DAPG, exhibits potent antibacterial properties by interacting with bacterial cell membranes and is useful for</p>

<p>Pexiganan acetate (MSI 78), a 22-residue peptide analogue of magainin 2, disrupts bacterial membranes or walls, leading to antibacterial activity.</p>

<p>Quorum Sensing-IN-2 (compound 23e) is a quorum sensing inhibitor that curtails bacterial pathogenicity without impeding growth.</p>

<p>WQ 2743 is a potent agent of antimicrobial.</p>

<p>DNA gyrase B-IN-3 (Compound A), with an IC50 of less than 10 nM, acts as an inhibitor of bacterial DNA gyrase B and exhibits antibacterial activity against Gram</p>

<p>Cefteram (T-2525), an orally active ester of the cephalosporin class, is the free acid form of Cefteram pivoxil.</p>

<p>Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide derived from bovine lactoferrin spanning residues 17-41, exhibits broad-spectrum antimicrobial properties against Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. Additionally, this compound demonstrates antitumor activities [1] [2].</p>

<p>Antituberculosis agent-6: potent against M. tuberculosis (MIC 3.49 μM), antifungal (MIC 62.5 μM), high GI absorption.</p>

<p>Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.</p>

<p>Acorafloxacin: broad-spectrum fluoroquinolone antibacterial for acute skin infections and pneumonia.</p>

<p>Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when</p>

<p>4-Aminosalicylic acid hemicalcium, an orally active antibiotic, shows potential in tuberculosis research [1].</p>

<p>Sulfachloropyridazine (sodium) is a sulfonamide antibiotic that impedes bacterial proliferation [1].</p>

<p>Beta-gal-nonoate, a β-galactosidase dependent nitric oxide (NO) donor, releases NO upon activation by β-galactosidase. It exhibits bactericidal activity, thus serving as an effective bactericide [1].</p>

<p>Daldinone A (Compound 4), isolated from Nigrospora oryzae, exhibits antibacterial properties, specifically demonstrating antimicrobial potential against P. aeruginosa [1].</p>

<p>Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).</p>

<p>Photosensitizer-1 shows promise in treating infections, effective against S. aureus in mouse wounds.</p>

<p>DNA Gyrase-IN-8 is a potent inhibitor of DNA gyrase, demonstrating antimicrobial activity with an IC50 of 8.45 µM [1].</p>

<p>AB131, an inhibitor of MSMEG 6649 and Rv2172c (KD values of 0.16 and 0.02 μM, respectively), enhances the antimycobacterial efficacy of the antitubercular agent</p>

<p>Contezolid (MRX-I) is an antibiotic with bactericidal activity and can be used to study tuberculosis.</p>

<p>Salicyl-AMS is an inhibitor of mycobacterium auxin biosynthesis that inhibits the growth of mycobacterium in the presence of iron deficiency in vitro.</p>

<p>A7132 is an antibacterial agent and possesses broad and potent antibacterial activity.</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>Antibacterial agent 76 (compound 9) is a potent antibacterial agent.</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>G247 inhibits MsbA by keeping NBDs apart, blocking ATPase activity.</p>

<p>Antibacterial agent 82 (compound 7p) is an antibacterial agent [1].</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>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>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>TB inhibitor 4, a spirothiazolidinone from mandelic acid, blocks 98% of M. tuberculosis H37Rv under 6 μg/mL.</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>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>Aztreonam-siderophore conjugate 63 is an antibacterial agent that exhibits efficacy against Gram-negative bacteria through the linkage of aztreonam to a</p>

<p>8-Hydroxyerythromycin A is a semi-synthetic antibiotic with antibacterial activity.</p>

<p>vacuolar H+-ATPases (V-ATPases) inhibitor</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>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>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>(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>

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

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

<p>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).</p>

<p>QPX7728 methoxy acetoxy methy ester is an inhibitor of boronic acid β-lactamase.</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>GT-055 (LCB18-055) is a novel inhibitor of broad-spectrum β-lactamase.</p>

<p>PqsR-IN-1, potent PqsR inhibitor, curbs pyocyanin in Pseudomonas aeruginosa with low cytotoxicity.</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>BWC0977 is an effective topoisomerase inhibitor that disrupts bacterial DNA replication by targeting both DNA gyrase and topoisomerase IV. The minimum inhibitory concentration (MIC90) of BWC0977 against MDR (multi-drug resistant) Gram-negative bacteria ranges from 0.03 to 2 µg/mL.</p>

<p>Fabimycin, a FabI inhibitor, combats drug-resistant gram-negative bacterial infections effectively.</p>

<p>NBTIs-IN-4, a broad-spectrum Gram-positive antibacterial, inhibits DNA rotamases/topoisomerase IV, with low resistance.</p>

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

<p>8-Deazafolic acid inhibits folate-dependent bacteria S. faecium &amp; L. casei, and fights lymphoid leukemia L1210 in mice.</p>