Antibatterico

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

<p>8-Hydroxyerythromycin A is a semi-synthetic antibiotic with antibacterial activity.</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>Antibacterial agent 82 (compound 7p) is an antibacterial agent [1].</p>

<p>G247 inhibits MsbA by keeping NBDs apart, blocking ATPase activity.</p>

<p>TB inhibitor 4, a spirothiazolidinone from mandelic acid, blocks 98% of M. tuberculosis H37Rv under 6 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>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>(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>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>Squalamine lactate is an aminosterol compound discovered in the tissues of the dogfish shark, with antimicrobial activity.</p>

<p>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.</p>

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

<p>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.</p>

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

<p>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.</p>

<p>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].</p>

<p>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.</p>

<p>β-Glucuronidase-IN-2 is a potent inhibitor of E.</p>

<p>Pisiferic acid is a novel PP2C activator and an an antimicrobial diterpenoid</p>

<p>Compound 6q, a trifluoromethylpyridine oxadiazole, targets Xanthomonas oryzae with EC50 of 7.2 μg/mL.</p>

<p>Eravacycline (TP-434) is a potent and broad-spectrum antibacterial agent.</p>

<p>MsbA-IN-3 is a potent and highly selective MsbA inhibitor (IC50: 2 nM). MsbA-IN-3 inhibits Escherichia coli activity (MIC: 35 μM).</p>

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

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

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

<p>Cetefloxacin (E 4868) is a broad-spectrum antibacterial antibiotic with a minimum inhibitory concentration (MIC) ranging from 0.007 to 8 µg/ml. In mice, cetefloxacin demonstrates favorable pharmacokinetic properties and provides protection against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.</p>

<p>Cefoxazole is a β-lactam antibiotic featuring an isoxazole structure, known for its antibacterial activity. It can be utilized in the study of infectious diseases.</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>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>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>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>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>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>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>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>