Antibacterial

7-Hydroxytropolone (3-Hydroxytropolone) is an antibiotic that exhibits activity against Gram-positive and Gram-negative bacteria, as well as yeasts and fungi. It also functions as an inhibitor of 2''-O-adenylate transferase.

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

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.

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].

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.

Compound 6xa inhibits drug-resistant tuberculosis with MICs 0.03 μg/mL for DS-Mtb and 0.03-0.06 for DR-Mtb, SI>40 for Vero cells.

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).

Citric acid-13C2 is a 13C-labeled form of citric acid. Citric acid serves as a preservative and food additive. It induces apoptosis in HaCaT cells and causes cell cycle arrest at the G2/M and S phases. Additionally, citric acid contributes to liver oxidative damage by reducing antioxidant enzyme activity. It also functions as an acidulant, emulsifier, chelating agent, and buffer, with extensive applications across multiple industries.

SPR719 is an inhibitor of gyrase B, has bactericidal activity.

Vitamin K5 (hydrochloride), a naphthoquinone compound, exhibits trichomonacidal activity in vitro and can be utilized for anti-infection research [1].

Antibacterialagent 278 (compound B1) is an antimicrobial agent that exhibits potent inhibitory activity against Gram-positive bacteria.

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.

MtTMPK-IN-9 moderately inhibits MtbTMPK (IC50: 48 μM), has submicromolar Mycobacterium activity, and is non-toxic, aiding tuberculosis research.

10(R)-hydroxy Stearic acid is a hydroxy fatty acid resulting from the hydroxylation of oleic acid, produced by gut microbiota.

Compound 7b (Antibacterial agent 99) is an effective agent with antibacterial, antifungal properties and no haemolytic activity.

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.

Antibacterial agent 81 blocks DNA transcription, targets S. aureus (MIC 12.5μM) & M. smegmatis (MIC 7.8μM). Used in infection research.

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

MT0703 is a cephalosporin antibiotic featuring an aminothiazolylglycyl moiety with a 1,5-dihydroxy-4-pyridinone-2-carbonyl group, displaying potent activity against Pseudomonas species.

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.

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.

PROTACeDHFR Degrader-2 (compound 7b) is an effective degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), capable of reliably degrading eDHFR-tagged proteins.

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.

(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

Lambertellin, an effective antibiotic, acts as both a bactericide and fungicide. It exerts anti-inflammatory effects in LPS-stimulated RAW 264.7 macrophages by modulating the activation of MAPK and NF-κB signaling pathways.

O-1269 acts as a partial agonist for the cannabinoid receptor 1 (CB1R), with a binding affinity (Ki) of 32 nM. Additionally, it exhibits analgesic properties.

Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma.

Antibacterial agent 88 is an effective antibacterial agent against B. subtilis (MIC: 4 μg/ml) with MIC values of ≤0.0156 μg/mL for MRSA, MRSE and S. aureus.

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

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.

Xeruborbactam isoboxil is a β-lactamase (beta-lactamase) inhibitor.

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.

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.

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.

L 689065 is a 5-lipoxygenase inhibitor.

Compound 5q is a potent antitubercular with low MIC90 values (0.40-23.51 μg/mL) against M. tuberculosis strains, showing minimal cytotoxicity.

DNA Gyrase-IN-1: potent, selective promoter inhibitor. IC50: 2.6 μM, inhibits Mtb, MIC: 0.49 μM. Useful for tuberculosis research.

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].

Elongation factor P-IN-2, a β-lysine derivative, is a potent EFP inhibitor reducing E. coli growth.

ACHN-975: potent LpxC inhibitor with subnanomolar activity; targets many gram-negative bacteria; MIC ≤1 μg/mL.

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

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].

Antibacterial agent 76 (compound 9) is a potent antibacterial agent.

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

Antibacterialagent 262 (compound A23) is a potent antibacterial agent that inhibits the activity of Xanthomonas oryzae pv oryzae. It also disrupts the integrity of bacterial cell membranes by preventing the formation of biofilms of Xanthomonas oryzae pv oryzae.

Antibacterial agent 75 re-sensitizes VRSA to vancomycin.

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.

RNAP-σ interaction inhibitor-2 (compound 7d) is an inhibitor targeting the interaction between RNA polymerase and the sigma factor. It demonstrates inhibitory activity against S. aureus with a minimum inhibitory concentration (MIC) of 2 µg/mL.

WQ3810 is an orally active fluoroquinolone, has potent antibacterial activities.

Anti-MRSA agent 3 targets MRSA with 0.098 μg/ml MIC, low toxicity, binds DNA, and disrupts cell walls/membranes.

GT-055 (LCB18-055) is a novel inhibitor of broad-spectrum β-lactamase.

Antibacterial agent 79 is an antibacterial agent.

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).

H2S scavenger 1 triflate (Compound 7b) serves as a selective H2S depleting agent, particularly against glutathione. This compound impedes the formation of bacterial biofilms and enhances the sensitivity of Staphylococcus aureus to gentamicin or photosensitizers by depleting H2S.

1,5-Dideoxy-1,5-imino-D-mannitol is an antibiotic with antibacterial properties.

8-Deazafolic acid inhibits folate-dependent bacteria S. faecium & L. casei, and fights lymphoid leukemia L1210 in mice.

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

Thiolactomycin is a novel reversible dual inhibitor of D-amino acid oxidase (DAO) and D-Aspartate oxidase (DDO).

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

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].

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

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.

Kikumycin A, an antibiotic produced by Streptomyces, exhibits antimicrobial activity against both Gram-positive and Gram-negative bacteria. Additionally, it demonstrates antitrichomonal activity with a minimum inhibitory concentration (MIC) of 25 μg/mL against Trichomonas foetus.

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

VEGFR-2/DHFR-IN-2 inhibits VEGFR-2 & DHFR (IC50: 0.623 & 9.085 μM), toxic to C26, HepG2, MCF7 cells (IC50: 3.59-8.38 μM), promising for cancer study.

Isotodesnitazene is an opioid compound that primarily targets the μ-opioid receptor (MOR). It exhibits EC50 values of 34.8 nM and 142 nM for MOR-βarr2 and MOR-mini-Gi, respectively. Isotodesnitazene can be utilized for research in opioid drugs.

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.

Rubropunctatin is a monascus pigment with very potent cancer cell proliferation inhibitory effects.

Antibacterial agent 113 targets multiple bacteria including P. aeruginosa and E. coli, showing efficacy at MIC 15625 μM.

DRF-8417 is an oxazolidinone antibiotic, active against both Gram-positive bacteria and fastidious Gram-negative bacteria. The MIC50 and MIC90 values of DRF-8417 for Gram-positive pathogens range between 0.06-1 mg/L.

NS-062 is an orally effective, irreversible covalent inhibitor targeting EGFR, demonstrating antiproliferative activity in the resistant double mutant H1975 cells with an IC50 of 0.19 μM. It also exhibits antitumor activity in a murine H1975 xenograft model.

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].

CM-728 is an oxazanonaphthoquinone that exhibits cytotoxic and antibacterial properties. It acts as a human peroxidase-1 inhibitor and serves as a source of oxidative stress affecting mitochondrial function.

DNA ligase-IN-2 (compound 2) acts as a potent LigA inhibitor, effectively hindering the DNA-independent spontaneous adenylation activity of full-length LigA and the truncated enzyme LigA:AD with an IC50 of 29 nM. It also significantly suppresses the in vitro growth of Staphylococcus aureus, showing MIC values of 1 μg/mL for S. aureus ATCC 29213 and S. aureus ATCC 700699, while the MIC for Escherichia coli (E. coli) ATCC 25922 is >64 μg/mL.

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

DNA Gyrase-IN-13 (compound 1b) is an inhibitor of DNA gyrase with bacteriostatic properties. It exhibits an IC50 of 1.81 μM against Staphylococcus aureus DNA gyrase.

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).

MBX-1162, a bis-indole compound, has demonstrated unique substrate specificity related to MepA and MepR in studies investigating its resistance mechanisms in Staphylococcus aureus. It has not shown cross-resistance with related compounds.

(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.

RmlA-IN-2: Strong RmlA blocker, hinders l-rhamnose synthesis & alters bacterial wall permeability (IC50: 0.303 μM).

Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.

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].

Antibacterial agent 118, potent against various mycobacteria, has MIC values ranging from 10.2 to 163.0 μM. Useful in TB research.

LpxC-IN-10 is a selective LpxC inhibitor with an MIC of 0.5 μg/mL against E. coli and K. pneumoniae and is capable of being used to study bacterial infections.

Cephalosporin C exhibits relatively weak resistance to Gram-positive and Gram-negative bacteria. It is stable against penicillinase, but can be decomposed by cephalosporinase. When hydrolyzed to remove its side chain, it yields 7-amino-cefenoic acid (7-ACA), which is an essential raw material for the production of semisynthetic cephalosporins.

ACHN-975 TFA is a selective inhibitor of the bacterial enzyme LpxC, antimicrobial against multiple Gram-negative bacteria.

QPX7728 methoxy acetoxy methy ester is an inhibitor of boronic acid β-lactamase.

vacuolar H+-ATPases (V-ATPases) inhibitor

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.

8-Hydroxyerythromycin A is a semi-synthetic antibiotic with antibacterial activity.

Dioxidine is an antimicrobial agent that can inhibit bacterial growth. It is utilized in research on pyogenic infections.

14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase with antibacterial activity.

Finafloxacin is a pH-activated fluoroquinolone, most effective at pH 5.0-6.0, targeting bacterial topoisomerases, used for UTIs and H. pylori infections.

Alpibectir has antibacterial activity [1].

Antibacterial agent 82 (compound 7p) is an antibacterial agent [1].

G247 inhibits MsbA by keeping NBDs apart, blocking ATPase activity.

LasR-IN-3 inhibits LasR in Pseudomonas, disrupting its dimer, causing loss of function.

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].